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Identification
NameClozapine
Accession NumberDB00363  (APRD00470)
TypeSmall Molecule
GroupsApproved
Description

A tricyclic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent. [PubChem]

Structure
Thumb
Synonyms
Clozapin
Clozapina
Clozapine
Clozapinum
External Identifiers
  • HF 1854
  • LX 100-129
  • W 108
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Auro-clozapinetablet200 mgoralAuro Pharma IncNot applicableNot applicableCanada
Auro-clozapinetablet100 mgoralAuro Pharma IncNot applicableNot applicableCanada
Auro-clozapinetablet50 mgoralAuro Pharma IncNot applicableNot applicableCanada
Auro-clozapinetablet25 mgoralAuro Pharma IncNot applicableNot applicableCanada
Clozapinetablet, orally disintegrating200 mg/1oralTeva Pharmaceuticals USA Inc2015-05-05Not applicableUs
Clozapinetablet, orally disintegrating150 mg/1oralTeva Pharmaceuticals USA Inc2015-05-05Not applicableUs
Clozapinetablet, orally disintegrating25 mg/1oralTeva Pharmaceuticals USA Inc2012-08-30Not applicableUs
Clozapinetablet, orally disintegrating12.5 mg/1oralTeva Pharmaceuticals USA Inc2012-08-30Not applicableUs
Clozapinetablet, orally disintegrating100 mg/1oralTeva Pharmaceuticals USA Inc2012-08-30Not applicableUs
Clozariltablet100 mgoralHls Therapeutics Inc1991-12-31Not applicableCanada
Clozariltablet100 mg/1oralCardinal Health1989-09-30Not applicableUs
Clozariltablet25 mg/1oralNovartis Pharmaceuticals Corporation1989-09-30Not applicableUs
Clozariltablet25 mgoralHls Therapeutics Inc1991-12-31Not applicableCanada
Clozariltablet25 mg/1oralTYA Pharmaceuticals1989-09-30Not applicableUs
Clozariltablet100 mg/1oralNovartis Pharmaceuticals Corporation1989-09-30Not applicableUs
Fazaclotablet, orally disintegrating200 mg/1oralJazz Pharmaceuticals, Inc.2010-07-09Not applicableUs
Fazaclotablet, orally disintegrating150 mg/1oralJazz Pharmaceuticals, Inc.2010-07-09Not applicableUs
Fazaclotablet, orally disintegrating100 mg/1oralJazz Pharmaceuticals, Inc.2008-06-01Not applicableUs
Fazaclotablet, orally disintegrating25 mg/1oralJazz Pharmaceuticals, Inc.2008-06-01Not applicableUs
Fazaclotablet, orally disintegrating12.5 mg/1oralJazz Pharmaceuticals, Inc.2007-07-01Not applicableUs
Gen-clozapinetablet25 mgoralMylan Pharmaceuticals Ulc2003-03-14Not applicableCanada
Gen-clozapinetablet200 mgoralMylan Pharmaceuticals Ulc2008-02-05Not applicableCanada
Gen-clozapinetablet50 mgoralMylan Pharmaceuticals Ulc2008-02-05Not applicableCanada
Gen-clozapinesuspension50 mgoralMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Gen-clozapinetablet100 mgoralMylan Pharmaceuticals Ulc2003-03-14Not applicableCanada
PMS-clozapinetablet100 mgoralPharmascience Inc2003-03-052011-01-20Canada
PMS-clozapinetablet25 mgoralPharmascience Inc2003-03-052011-01-20Canada
Sandoz Clozapinetablet25 mgoralSandoz Canada IncorporatedNot applicableNot applicableCanada
Sandoz Clozapinetablet100 mgoralSandoz Canada IncorporatedNot applicableNot applicableCanada
Versaclozsuspension50 mg/mLoralJazz Pharmaceuticals, Inc.2013-02-15Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-clozapinetablet100 mgoralApotex Inc2004-01-27Not applicableCanada
Apo-clozapinetablet25 mgoralApotex Inc2004-01-27Not applicableCanada
Clozapinetablet25 mg/1oralMylan Institutional Inc.1999-11-15Not applicableUs
Clozapinetablet100 mg/1oralCardinal Health2010-02-12Not applicableUs
Clozapinetablet25 mg/1oralTeva Pharmaceuticals USA Inc2007-05-10Not applicableUs
Clozapinetablet100 mg/1oralAvera Mc Kennan Hospital2015-08-12Not applicableUs
Clozapinetablet50 mg/1oralMylan Pharmaceuticals Inc.2010-04-20Not applicableUs
Clozapinetablet200 mg/1oralMylan Institutional Inc.2010-07-06Not applicableUs
Clozapinetablet100 mg/1oralAccord Healthcare Inc.2016-03-01Not applicableUs
Clozapinetablet100 mg/1oralMylan Pharmaceuticals Inc.1999-07-08Not applicableUs
Clozapinetablet100 mg/1oralActavis Pharma, Inc.2015-12-22Not applicableUs
Clozapinetablet25 mg/1oralAccord Healthcare Inc.2016-03-01Not applicableUs
Clozapinetablet25 mg/1oralMylan Pharmaceuticals Inc.1999-07-08Not applicableUs
Clozapinetablet25 mg/1oralActavis Pharma, Inc.2015-12-22Not applicableUs
Clozapinetablet100 mg/1oralTeva Pharmaceuticals USA Inc2009-09-18Not applicableUs
Clozapinetablet100 mg/1oralSun Pharmaceutical Industries, Inc.2002-11-15Not applicableUs
Clozapinetablet, orally disintegrating100 mg/1oralMylan Pharmaceuticals Inc.2015-11-02Not applicableUs
Clozapinetablet200 mg/1oralTeva Pharmaceuticals USA Inc2007-05-15Not applicableUs
Clozapinetablet25 mg/1oralSun Pharmaceutical Industries, Inc.2002-11-15Not applicableUs
Clozapinetablet, orally disintegrating25 mg/1oralMylan Pharmaceuticals Inc.2015-11-02Not applicableUs
Clozapinetablet100 mg/1oralMylan Institutional Inc.1999-11-15Not applicableUs
Clozapinetablet50 mg/1oralSun Pharmaceutical Industries, Inc.2005-08-19Not applicableUs
Clozapinetablet50 mg/1oralTeva Pharmaceuticals USA Inc2007-03-19Not applicableUs
Clozapinetablet200 mg/1oralMylan Pharmaceuticals Inc.2010-04-20Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AzaleptineArpimed
ClomentPharmaplan
ClonexAdeka
ClopinEast West
ClopineDouglas
ClopsinePsicofarma
ClorazemRemedica
LanoleptLannacher
LapenaxNovartis
LeponexNovartis
LoduxRider
LozapinTorrent
LuftenPharos
MezapinPanbiotic
RefractCrescent
RefraxolAC Farma
SensipinBeximco
SequaxIvax
SizopinSun
SizoprilMeprofarm
SyclopBrown & Burk Phils
SyzopinPsyco Remedies
TanylNovamed
UspenYu Sheng
ZapenPsipharma
ZapeniaIncepta
ZapineTaiwan Biotech
ZiprocTorrent
ZopinPsychotropics India
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIJ60AR2IKIC
CAS number5786-21-0
WeightAverage: 326.823
Monoisotopic: 326.129824335
Chemical FormulaC18H19ClN4
InChI KeyQZUDBNBUXVUHMW-UHFFFAOYSA-N
InChI
InChI=1S/C18H19ClN4/c1-22-8-10-23(11-9-22)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,20H,8-11H2,1H3
IUPAC Name
6-chloro-10-(4-methylpiperazin-1-yl)-2,9-diazatricyclo[9.4.0.0³,⁸]pentadeca-1(15),3,5,7,9,11,13-heptaene
SMILES
CN1CCN(CC1)C1=NC2=CC(Cl)=CC=C2NC2=CC=CC=C12
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as dibenzodiazepines. These are compounds containing a dibenzodiazepine moiety, which consists of two benzene connected by a diazepine ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzodiazepines
Sub ClassDibenzodiazepines
Direct ParentDibenzodiazepines
Alternative Parents
Substituents
  • Dibenzodiazepine
  • 1,4-benzodiazepine
  • N-alkylpiperazine
  • N-methylpiperazine
  • Chlorobenzene
  • Imidolactam
  • Benzenoid
  • Piperazine
  • 1,4-diazinane
  • Aryl halide
  • Aryl chloride
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Secondary amine
  • Carboxylic acid amidine
  • Amidine
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor use in patients with treatment-resistant schizophrenia.
PharmacodynamicsClozapine is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives and is indicated for the treatment of schizophrenia. Clozapine is a selective monoaminergic antagonist with high affinity for the serotonin Type 2 (5HT2), dopamine Type 2 (D2), 1 and 2 adrenergic, and H1 histaminergic receptors. Clozapine acts as an antagonist at other receptors, but with lower potency. Antagonism at receptors other than dopamine and 5HT2 with similar receptor affinities may explain some of the other therapeutic and side effects of Clozapine. Clozapine's antagonism of muscarinic M1-5 receptors may explain its anticholinergic effects. Clozapine's antagonism of histamine H1 receptors may explain the somnolence observed with this drug. Clozapine's antagonism of adrenergic a1 receptors may explain the orthostatic hypotension observed with this drug.
Mechanism of actionClozapine's antipsychotic action is likely mediated through a combination of antogistic effects at D2 receptors in the mesolimbic pathway and 5-HT2A receptors in the frontal cortex. D2 antagonism relieves positive symptoms while 5-HT2A antagonism alleviates negative symptoms.
Related Articles
AbsorptionRapid and almost complete
Volume of distributionNot Available
Protein binding97% (bound to serum proteins)
Metabolism

Hepatic

SubstrateEnzymesProduct
Clozapine
NorclozapineDetails
Clozapine
Clozapine N-oxideDetails
Clozapine
Clozapine glucuronideDetails
Route of eliminationApproximately 50% of the administered dose is excreted in the urine and 30% in the feces.
Half life8 hours (range 4-12 hours)
ClearanceNot Available
ToxicityClozapine carries a black-box warning for agranulocytosis.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug Reactions
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeAdverse ReactionReference(s)
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-3
Gene symbol: GNB3
UniProt: P16520
rs5443 Not AvailableTT alleleSchizophrenia patients taking this drug more more weight than patients with at least one rs5443(c) allele16141801
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9904
Blood Brain Barrier+0.9614
Caco-2 permeable+0.6151
P-glycoprotein substrateSubstrate0.8684
P-glycoprotein inhibitor IInhibitor0.6791
P-glycoprotein inhibitor IIInhibitor0.7407
Renal organic cation transporterInhibitor0.8049
CYP450 2C9 substrateNon-substrate0.7509
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateSubstrate0.6088
CYP450 1A2 substrateInhibitor0.5722
CYP450 2C9 inhibitorNon-inhibitor0.9432
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.9137
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.571
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.9106
BiodegradationNot ready biodegradable1.0
Rat acute toxicity3.0838 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8189
hERG inhibition (predictor II)Inhibitor0.7164
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Azur pharma international iii ltd
  • Caraco pharmaceutical laboratories ltd
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Mylan pharmaceuticals inc
  • Par pharmaceutical
  • Sandoz inc
  • Novartis pharmaceuticals corp
Packagers
Dosage forms
FormRouteStrength
Tabletoral200 mg/1
Tabletoral50 mg/1
Tablet, orally disintegratingoral100 mg/1
Tablet, orally disintegratingoral12.5 mg/1
Tablet, orally disintegratingoral150 mg/1
Tablet, orally disintegratingoral200 mg/1
Tablet, orally disintegratingoral25 mg/1
Tabletoral100 mg/1
Tabletoral25 mg/1
Suspensionoral50 mg
Tabletoral100 mg
Tabletoral200 mg
Tabletoral25 mg
Tabletoral50 mg
Suspensionoral50 mg/mL
Prices
Unit descriptionCostUnit
Fazaclo 100 mg odt6.55USD tablet
Clozapine 200 mg tablet6.32USD tablet
Clozaril 100 mg tablet5.84USD tablet
Clozapine 100 mg tablet3.33USD tablet
Apo-Clozapine 100 mg Tablet2.77USD tablet
Gen-Clozapine 100 mg Tablet2.77USD tablet
Fazaclo 25 mg odt2.4USD tablet
Fazaclo 25 mg tablet2.19USD tablet
Clozaril 25 mg tablet1.96USD tablet
Fazaclo 12.5 mg odt1.79USD tablet
Clozapine 50 mg tablet1.65USD tablet
Clozapine 25 mg tablet1.28USD tablet
Apo-Clozapine 25 mg Tablet0.69USD tablet
Gen-Clozapine 25 mg Tablet0.69USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5178878 No1993-01-122010-01-12Us
US6024981 No1998-04-092018-04-09Us
US6106861 No1997-12-052017-12-05Us
US6221392 No1998-04-092018-04-09Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point183-184 °CPhysProp
water solubility11.8 mg/LNot Available
logP3.23HANSCH,C ET AL. (1995)
pKa7.5EL TAYAR,N ET AL. (1985)
Predicted Properties
PropertyValueSource
Water Solubility0.186 mg/mLALOGPS
logP3.67ALOGPS
logP3.4ChemAxon
logS-3.2ALOGPS
pKa (Strongest Acidic)15.9ChemAxon
pKa (Strongest Basic)7.35ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area30.87 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity97.36 m3·mol-1ChemAxon
Polarizability35.77 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
References
Synthesis Reference

Schmutz, J. and Hunziker, F.; US. Patent 3,539,573; November 10, 1970 .

US3539573
General References
  1. Alvir JM, Lieberman JA, Safferman AZ, Schwimmer JL, Schaaf JA: Clozapine-induced agranulocytosis. Incidence and risk factors in the United States. N Engl J Med. 1993 Jul 15;329(3):162-7. [PubMed:8515788 ]
  2. Vaddadi KS, Soosai E, Vaddadi G: Low blood selenium concentrations in schizophrenic patients on clozapine. Br J Clin Pharmacol. 2003 Mar;55(3):307-9. [PubMed:12630982 ]
  3. Naheed M, Green B: Focus on clozapine. Curr Med Res Opin. 2001;17(3):223-9. [PubMed:11900316 ]
  4. Lane HY, Chang YC, Chang WH, Lin SK, Tseng YT, Jann MW: Effects of gender and age on plasma levels of clozapine and its metabolites: analyzed by critical statistics. J Clin Psychiatry. 1999 Jan;60(1):36-40. [PubMed:10074876 ]
External Links
ATC CodesN05AH02
AHFS Codes
  • 28:16.08.04
PDB EntriesNot Available
FDA labelDownload (89.8 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Clozapine can be increased when it is combined with Abiraterone.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Clozapine.
AclidiniumAclidinium may increase the anticholinergic activities of Clozapine.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Clozapine.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Clozapine.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Clozapine.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Clozapine.
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Clozapine.
AltretamineThe risk or severity of adverse effects can be increased when Altretamine is combined with Clozapine.
AmisulprideThe risk or severity of adverse effects can be increased when Clozapine is combined with Amisulpride.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Clozapine.
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Clozapine.
AmphetamineClozapine may decrease the stimulatory activities of Amphetamine.
AmsacrineThe risk or severity of adverse effects can be increased when Amsacrine is combined with Clozapine.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Clozapine.
Arsenic trioxideThe risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Clozapine.
AzacitidineThe risk or severity of adverse effects can be increased when Azacitidine is combined with Clozapine.
AzelastineClozapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Clozapine.
BelinostatThe risk or severity of adverse effects can be increased when Belinostat is combined with Clozapine.
BendamustineThe risk or severity of adverse effects can be increased when Bendamustine is combined with Clozapine.
BenzphetamineClozapine may decrease the stimulatory activities of Benzphetamine.
BevacizumabThe risk or severity of adverse effects can be increased when Bevacizumab is combined with Clozapine.
BexaroteneThe risk or severity of adverse effects can be increased when Bexarotene is combined with Clozapine.
BlinatumomabThe risk or severity of adverse effects can be increased when Blinatumomab is combined with Clozapine.
BortezomibThe risk or severity of adverse effects can be increased when Bortezomib is combined with Clozapine.
BosutinibThe risk or severity of adverse effects can be increased when Bosutinib is combined with Clozapine.
Botulinum Toxin Type AClozapine may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BClozapine may increase the anticholinergic activities of Botulinum Toxin Type B.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Clozapine.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Clozapine.
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Clozapine.
BromocriptineThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Clozapine.
BuprenorphineClozapine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Clozapine.
BusulfanThe risk or severity of adverse effects can be increased when Busulfan is combined with Clozapine.
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Clozapine.
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Clozapine.
CamazepamThe risk or severity of adverse effects can be increased when Camazepam is combined with Clozapine.
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Clozapine.
CapecitabineThe risk or severity of adverse effects can be increased when Capecitabine is combined with Clozapine.
CarbamazepineCarbamazepine may increase the myelosuppressive activities of Clozapine.
CarboplatinThe risk or severity of adverse effects can be increased when Carboplatin is combined with Clozapine.
CarfilzomibThe risk or severity of adverse effects can be increased when Carfilzomib is combined with Clozapine.
CarmustineThe risk or severity of adverse effects can be increased when Carmustine is combined with Clozapine.
CathinoneClozapine may decrease the stimulatory activities of Cathinone.
ChlorambucilThe risk or severity of adverse effects can be increased when Chlorambucil is combined with Clozapine.
ChloramphenicolThe risk or severity of adverse effects can be increased when Chloramphenicol is combined with Clozapine.
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Clozapine.
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Clozapine.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Clozapine.
CimetidineThe serum concentration of Clozapine can be increased when it is combined with Cimetidine.
Cimetropium BromideClozapine may increase the anticholinergic activities of Cimetropium Bromide.
CinolazepamThe risk or severity of adverse effects can be increased when Cinolazepam is combined with Clozapine.
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Clozapine.
CisplatinThe risk or severity of adverse effects can be increased when Cisplatin is combined with Clozapine.
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Clozapine.
CladribineThe risk or severity of adverse effects can be increased when Cladribine is combined with Clozapine.
ClarithromycinThe metabolism of Clozapine can be decreased when combined with Clarithromycin.
ClobazamThe risk or severity of adverse effects can be increased when Clobazam is combined with Clozapine.
ClofarabineThe risk or severity of adverse effects can be increased when Clofarabine is combined with Clozapine.
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Clozapine.
ClonazepamThe risk or severity of adverse effects can be increased when Clonazepam is combined with Clozapine.
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Clozapine.
ClotiazepamThe risk or severity of adverse effects can be increased when Clotiazepam is combined with Clozapine.
CloxazolamThe risk or severity of adverse effects can be increased when Cloxazolam is combined with Clozapine.
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Clozapine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Clozapine.
CyclophosphamideThe risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Clozapine.
Cyproterone acetateThe serum concentration of Clozapine can be decreased when it is combined with Cyproterone acetate.
CytarabineThe risk or severity of adverse effects can be increased when Cytarabine is combined with Clozapine.
DacarbazineThe risk or severity of adverse effects can be increased when Dacarbazine is combined with Clozapine.
DactinomycinThe risk or severity of adverse effects can be increased when Dactinomycin is combined with Clozapine.
DasatinibThe risk or severity of adverse effects can be increased when Dasatinib is combined with Clozapine.
DaunorubicinThe risk or severity of adverse effects can be increased when Daunorubicin is combined with Clozapine.
DecitabineThe risk or severity of adverse effects can be increased when Decitabine is combined with Clozapine.
DeferasiroxThe serum concentration of Clozapine can be increased when it is combined with Deferasirox.
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Clozapine.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Desvenlafaxine is combined with Clozapine.
DexrazoxaneThe risk or severity of adverse effects can be increased when Dexrazoxane is combined with Clozapine.
DextroamphetamineClozapine may decrease the stimulatory activities of Dextroamphetamine.
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Clozapine.
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Clozapine.
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Clozapine.
DinutuximabThe risk or severity of adverse effects can be increased when Dinutuximab is combined with Clozapine.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Clozapine.
DofetilideClozapine may increase the QTc-prolonging activities of Dofetilide.
DonepezilDonepezil may increase the central neurotoxic activities of Clozapine.
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Clozapine.
DoxorubicinThe risk or severity of adverse effects can be increased when Doxorubicin is combined with Clozapine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Clozapine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Clozapine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Clozapine.
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Clozapine.
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Clozapine.
EluxadolineClozapine may increase the activities of Eluxadoline.
EnzalutamideThe serum concentration of Clozapine can be decreased when it is combined with Enzalutamide.
EpirubicinThe risk or severity of adverse effects can be increased when Epirubicin is combined with Clozapine.
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Clozapine.
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Clozapine.
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Clozapine.
EribulinThe risk or severity of adverse effects can be increased when Eribulin is combined with Clozapine.
ErythromycinThe metabolism of Clozapine can be decreased when combined with Erythromycin.
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Clozapine.
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Clozapine.
EthanolClozapine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EtoposideThe risk or severity of adverse effects can be increased when Etoposide is combined with Clozapine.
EverolimusThe risk or severity of adverse effects can be increased when Everolimus is combined with Clozapine.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Clozapine.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Clozapine.
FloxuridineThe risk or severity of adverse effects can be increased when Floxuridine is combined with Clozapine.
FlucytosineThe risk or severity of adverse effects can be increased when Flucytosine is combined with Clozapine.
FludarabineThe risk or severity of adverse effects can be increased when Fludarabine is combined with Clozapine.
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Clozapine.
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Clozapine.
FluorouracilThe risk or severity of adverse effects can be increased when Fluorouracil is combined with Clozapine.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Clozapine.
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Clozapine.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Clozapine.
FosphenytoinThe serum concentration of Clozapine can be decreased when it is combined with Fosphenytoin.
FrovatriptanThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Clozapine.
GalantamineGalantamine may increase the central neurotoxic activities of Clozapine.
GemcitabineThe risk or severity of adverse effects can be increased when Gemcitabine is combined with Clozapine.
Gemtuzumab ozogamicinThe risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Clozapine.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Clozapine.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Clozapine.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Clozapine.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Clozapine is combined with Glucagon recombinant.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Clozapine.
GoserelinGoserelin may increase the QTc-prolonging activities of Clozapine.
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Clozapine.
HydrocodoneClozapine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyureaThe risk or severity of adverse effects can be increased when Hydroxyurea is combined with Clozapine.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Clozapine.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Ibritumomab is combined with Clozapine.
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Clozapine.
IdarubicinThe risk or severity of adverse effects can be increased when Idarubicin is combined with Clozapine.
IfosfamideThe risk or severity of adverse effects can be increased when Ifosfamide is combined with Clozapine.
ImatinibThe risk or severity of adverse effects can be increased when Imatinib is combined with Clozapine.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Clozapine.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Clozapine.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Clozapine.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Clozapine.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Clozapine.
Insulin HumanThe therapeutic efficacy of Insulin Regular can be decreased when used in combination with Clozapine.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Clozapine.
Interferon alfa-n3The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Clozapine.
Interferon alfacon-1The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Clozapine.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Clozapine.
IrinotecanThe risk or severity of adverse effects can be increased when Irinotecan is combined with Clozapine.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Clozapine.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Clozapine.
IvabradineIvabradine may increase the QTc-prolonging activities of Clozapine.
IxabepiloneThe risk or severity of adverse effects can be increased when Ixabepilone is combined with Clozapine.
IxazomibThe risk or severity of adverse effects can be increased when Ixazomib is combined with Clozapine.
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with Clozapine.
L-PhenylalanineThe risk or severity of adverse effects can be increased when L-Phenylalanine is combined with Clozapine.
LenalidomideThe risk or severity of adverse effects can be increased when Lenalidomide is combined with Clozapine.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Clozapine.
LevomilnacipranThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Clozapine.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Clozapine.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Clozapine.
LisdexamfetamineClozapine may decrease the stimulatory activities of Lisdexamfetamine.
LithiumLithium may increase the neurotoxic activities of Clozapine.
LomustineThe risk or severity of adverse effects can be increased when Lomustine is combined with Clozapine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Clozapine.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Clozapine.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Clozapine.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Clozapine.
MechlorethamineThe risk or severity of adverse effects can be increased when Mechlorethamine is combined with Clozapine.
MelphalanThe risk or severity of adverse effects can be increased when Melphalan is combined with Clozapine.
MequitazineClozapine may increase the arrhythmogenic activities of Mequitazine.
MercaptopurineThe risk or severity of adverse effects can be increased when Mercaptopurine is combined with Clozapine.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Clozapine.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Clozapine.
MethamphetamineClozapine may decrease the stimulatory activities of Methamphetamine.
MethimazoleThe risk or severity of adverse effects can be increased when Methimazole is combined with Clozapine.
MethotrexateThe risk or severity of adverse effects can be increased when Methotrexate is combined with Clozapine.
MethotrimeprazineClozapine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethoxsalenThe serum concentration of Clozapine can be increased when it is combined with Methoxsalen.
MethylphenidateThe risk or severity of adverse effects can be increased when Clozapine is combined with Methylphenidate.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Clozapine.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Clozapine.
MetyrosineClozapine may increase the sedative activities of Metyrosine.
MexiletineThe serum concentration of Clozapine can be increased when it is combined with Mexiletine.
MianserinMianserin may increase the anticholinergic activities of Clozapine.
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Clozapine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Clozapine.
MilnacipranThe risk or severity of adverse effects can be increased when Milnacipran is combined with Clozapine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Clozapine.
MirabegronThe risk or severity of adverse effects can be increased when Clozapine is combined with Mirabegron.
MirtazapineClozapine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MitomycinThe risk or severity of adverse effects can be increased when Mitomycin is combined with Clozapine.
MitotaneThe serum concentration of Clozapine can be decreased when it is combined with Mitotane.
MitoxantroneThe risk or severity of adverse effects can be increased when Mitoxantrone is combined with Clozapine.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Clozapine.
MorphineThe risk or severity of adverse effects can be increased when Clozapine is combined with Morphine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Clozapine.
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Clozapine.
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Clozapine.
NefazodoneThe metabolism of Clozapine can be decreased when combined with Nefazodone.
NelarabineThe risk or severity of adverse effects can be increased when Nelarabine is combined with Clozapine.
NilotinibThe risk or severity of adverse effects can be increased when Nilotinib is combined with Clozapine.
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Clozapine.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Clozapine.
ObinutuzumabThe risk or severity of adverse effects can be increased when Obinutuzumab is combined with Clozapine.
OctreotideOctreotide may increase the QTc-prolonging activities of Clozapine.
OfloxacinThe serum concentration of Clozapine can be increased when it is combined with Ofloxacin.
OlaparibThe risk or severity of adverse effects can be increased when Olaparib is combined with Clozapine.
OmeprazoleThe serum concentration of Clozapine can be decreased when it is combined with Omeprazole.
OrphenadrineClozapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OsimertinibThe risk or severity of adverse effects can be increased when Osimertinib is combined with Clozapine.
OxaliplatinThe risk or severity of adverse effects can be increased when Oxaliplatin is combined with Clozapine.
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Clozapine.
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Clozapine.
PalbociclibThe risk or severity of adverse effects can be increased when Palbociclib is combined with Clozapine.
ParaldehydeClozapine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Paroxetine is combined with Clozapine.
Peginterferon alfa-2aThe risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Clozapine.
Peginterferon alfa-2bThe risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Clozapine.
PemetrexedThe risk or severity of adverse effects can be increased when Pemetrexed is combined with Clozapine.
PentostatinThe risk or severity of adverse effects can be increased when Pentostatin is combined with Clozapine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Clozapine.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Clozapine.
PhendimetrazineClozapine may decrease the stimulatory activities of Phendimetrazine.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Clozapine.
PhenobarbitalThe serum concentration of Clozapine can be decreased when it is combined with Phenobarbital.
PhentermineClozapine may decrease the stimulatory activities of Phentermine.
PhenytoinThe serum concentration of Clozapine can be decreased when it is combined with Phenytoin.
PomalidomideThe risk or severity of adverse effects can be increased when Pomalidomide is combined with Clozapine.
PonatinibThe risk or severity of adverse effects can be increased when Ponatinib is combined with Clozapine.
Potassium ChlorideClozapine may increase the ulcerogenic activities of Potassium Chloride.
PramlintidePramlintide may increase the anticholinergic activities of Clozapine.
PrimaquineThe serum concentration of Clozapine can be increased when it is combined with Primaquine.
PrimidoneThe serum concentration of Clozapine can be decreased when it is combined with Primidone.
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Clozapine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Clozapine.
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Clozapine.
PropylthiouracilThe risk or severity of adverse effects can be increased when Propylthiouracil is combined with Clozapine.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Clozapine.
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Clozapine.
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Clozapine.
RaltitrexedThe risk or severity of adverse effects can be increased when Raltitrexed is combined with Clozapine.
RamosetronClozapine may increase the activities of Ramosetron.
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Clozapine.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Clozapine.
RifabutinThe serum concentration of Clozapine can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Clozapine can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Clozapine can be decreased when it is combined with Rifapentine.
RituximabThe risk or severity of adverse effects can be increased when Rituximab is combined with Clozapine.
RivastigmineRivastigmine may increase the central neurotoxic activities of Clozapine.
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Clozapine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Clozapine.
RuxolitinibThe risk or severity of adverse effects can be increased when Ruxolitinib is combined with Clozapine.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Clozapine.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Clozapine.
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Clozapine.
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Clozapine.
SirolimusThe risk or severity of adverse effects can be increased when Sirolimus is combined with Clozapine.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Clozapine.
SorafenibThe risk or severity of adverse effects can be increased when Sorafenib is combined with Clozapine.
St. John's WortThe serum concentration of Clozapine can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Clozapine can be increased when it is combined with Stiripentol.
StreptozocinThe risk or severity of adverse effects can be increased when Streptozocin is combined with Clozapine.
SulpirideThe risk or severity of adverse effects can be increased when Clozapine is combined with Sulpiride.
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Clozapine.
SuvorexantClozapine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineThe therapeutic efficacy of Clozapine can be decreased when used in combination with Tacrine.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Clozapine.
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Clozapine resulting in a loss in efficacy.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Clozapine.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Clozapine.
TelithromycinThe metabolism of Clozapine can be decreased when combined with Telithromycin.
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Clozapine.
TemozolomideThe risk or severity of adverse effects can be increased when Temozolomide is combined with Clozapine.
TemsirolimusThe risk or severity of adverse effects can be increased when Temsirolimus is combined with Clozapine.
TeniposideThe risk or severity of adverse effects can be increased when Teniposide is combined with Clozapine.
TeriflunomideThe serum concentration of Clozapine can be decreased when it is combined with Teriflunomide.
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Clozapine.
ThalidomideClozapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Clozapine.
ThiotepaThe risk or severity of adverse effects can be increased when Thiotepa is combined with Clozapine.
TioguanineThe risk or severity of adverse effects can be increased when Tioguanine is combined with Clozapine.
TiotropiumClozapine may increase the anticholinergic activities of Tiotropium.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Clozapine.
TofacitinibThe risk or severity of adverse effects can be increased when Tofacitinib is combined with Clozapine.
TofisopamThe risk or severity of adverse effects can be increased when Tofisopam is combined with Clozapine.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Clozapine.
TopiramateThe risk or severity of adverse effects can be increased when Clozapine is combined with Topiramate.
TopotecanThe risk or severity of adverse effects can be increased when Topotecan is combined with Clozapine.
TositumomabThe risk or severity of adverse effects can be increased when Tositumomab is combined with Clozapine.
TrabectedinThe risk or severity of adverse effects can be increased when Trabectedin is combined with Clozapine.
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Clozapine.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Clozapine.
Trastuzumab emtansineThe risk or severity of adverse effects can be increased when ado-trastuzumab emtansine is combined with Clozapine.
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Clozapine.
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Clozapine.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Clozapine.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Clozapine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Clozapine.
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Clozapine.
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Clozapine.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Clozapine.
VinblastineThe risk or severity of adverse effects can be increased when Vinblastine is combined with Clozapine.
VindesineThe risk or severity of adverse effects can be increased when Vindesine is combined with Clozapine.
VinorelbineThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Clozapine.
VorinostatThe risk or severity of adverse effects can be increased when Vorinostat is combined with Clozapine.
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Clozapine.
ZidovudineThe risk or severity of adverse effects can be increased when Zidovudine is combined with Clozapine.
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Clozapine.
ZolpidemClozapine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Avoid alcohol.
  • Limit caffeine intake (may reduce clozapine matabolism).
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Potassium channel regulator activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name:
DRD2
Uniprot ID:
P14416
Molecular Weight:
50618.91 Da
References
  1. Green AI, Salomon MS, Brenner MJ, Rawlins K: Treatment of schizophrenia and comorbid substance use disorder. Curr Drug Targets CNS Neurol Disord. 2002 Apr;1(2):129-39. [PubMed:12769622 ]
  2. Weizman T, Pick CG, Backer MM, Rigai T, Bloch M, Schreiber S: The antinociceptive effect of amisulpride in mice is mediated through opioid mechanisms. Eur J Pharmacol. 2003 Oct 8;478(2-3):155-9. [PubMed:14575800 ]
  3. Young RM, Lawford BR, Barnes M, Burton SC, Ritchie T, Ward WK, Noble EP: Prolactin levels in antipsychotic treatment of patients with schizophrenia carrying the DRD2*A1 allele. Br J Psychiatry. 2004 Aug;185:147-51. [PubMed:15286066 ]
  4. Stonehouse AH, Jones FS: Bromocriptine and clozapine regulate dopamine 2 receptor gene expression in the mouse striatum. J Mol Neurosci. 2005;25(1):29-36. [PubMed:15781964 ]
  5. Takano A, Suhara T, Kusumi I, Takahashi Y, Asai Y, Yasuno F, Ichimiya T, Inoue M, Sudo Y, Koyama T: Time course of dopamine D2 receptor occupancy by clozapine with medium and high plasma concentrations. Prog Neuropsychopharmacol Biol Psychiatry. 2006 Jan;30(1):75-81. Epub 2005 Jul 22. [PubMed:16040180 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Virus receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
Molecular Weight:
52602.58 Da
References
  1. Goldstein JM: Quetiapine fumarate (Seroquel): a new atypical antipsychotic. Drugs Today (Barc). 1999 Mar;35(3):193-210. [PubMed:12973385 ]
  2. McDonald LM, Moran PM, Vythelingum GN, Joseph MH, Stephenson JD, Gray JA: Enhancement of latent inhibition by two 5-HT2A receptor antagonists only when given at both pre-exposure and conditioning. Psychopharmacology (Berl). 2003 Sep;169(3-4):321-31. Epub 2002 Aug 9. [PubMed:14530903 ]
  3. Broderick PA, Hope O, Okonji C, Rahni DN, Zhou Y: Clozapine and cocaine effects on dopamine and serotonin release in nucleus accumbens during psychostimulant behavior and withdrawal. Prog Neuropsychopharmacol Biol Psychiatry. 2004 Jan;28(1):157-71. [PubMed:14687870 ]
  4. Heiser P, Schulte E, Hausmann C, Becker R, Remschmidt H, Krieg JC, Vedder H: Effects of clozapine and its metabolites on the 5-HT2 receptor system in cortical and hippocampal cells in vitro. Prog Neuropsychopharmacol Biol Psychiatry. 2004 Mar;28(2):297-302. [PubMed:14751426 ]
  5. Reist C, Mazzanti C, Vu R, Fujimoto K, Goldman D: Inter-relationships of intermediate phenotypes for serotonin function, impulsivity, and a 5-HT2A candidate allele: His452Tyr. Mol Psychiatry. 2004 Sep;9(9):871-8. [PubMed:15037867 ]
  6. Leysen JE, Janssen PM, Megens AA, Schotte A: Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry. 1994 May;55 Suppl:5-12. [PubMed:7520908 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
DRD1
Uniprot ID:
P21728
Molecular Weight:
49292.765 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name:
DRD3
Uniprot ID:
P35462
Molecular Weight:
44224.335 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Sh3 domain binding
Specific Function:
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins which inhibit adenylyl cyclase. Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (By similarity).
Gene Name:
DRD4
Uniprot ID:
P21917
Molecular Weight:
48359.86 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Zhao AL, Zhao JP, Zhang YH, Xue ZM, Chen JD, Chen XG: Dopamine D4 receptor gene exon III polymorphism and interindividual variation in response to clozapine. Int J Neurosci. 2005 Nov;115(11):1539-47. [PubMed:16223700 ]
  3. Nakane M, Cowart MD, Hsieh GC, Miller L, Uchic ME, Chang R, Terranova MA, Donnelly-Roberts DL, Namovic MT, Miller TR, Wetter JM, Marsh K, Stewart AO, Brioni JD, Moreland RB: 2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist. Neuropharmacology. 2005 Jul;49(1):112-21. Epub 2005 Apr 1. [PubMed:15992586 ]
  4. Kuballa G, Nowak P, Labus L, Bortel A, Dabrowska J, Swoboda M, Kwiecinski A, Kostrzewa RM, Brus R: Central effects of nafadotride, a dopamine D3 receptor antagonist, in rats. Comparison with haloperidol and clozapine. Pharmacol Rep. 2005 Mar-Apr;57(2):161-9. [PubMed:15886414 ]
  5. Glatt SJ, Faraone SV, Tsuang MT: Schizophrenia is not associated with DRD4 48-base-pair-repeat length or individual alleles: results of a meta-analysis. Biol Psychiatry. 2003 Sep 15;54(6):629-35. [PubMed:13129658 ]
  6. Patel S, Chapman KL, Marston D, Hutson PH, Ragan CI: Pharmacological and functional characterisation of dopamine D4 receptors in the rat retina. Neuropharmacology. 2003 Jun;44(8):1038-46. [PubMed:12763097 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
Molecular Weight:
46106.335 Da
References
  1. Hagino Y, Watanabe M: Effects of clozapine on the efflux of serotonin and dopamine in the rat brain: the role of 5-HT1A receptors. Can J Physiol Pharmacol. 2002 Dec;80(12):1158-66. [PubMed:12564641 ]
  2. Chou YH, Halldin C, Farde L: Occupancy of 5-HT1A receptors by clozapine in the primate brain: a PET study. Psychopharmacology (Berl). 2003 Mar;166(3):234-40. Epub 2003 Feb 13. [PubMed:12589516 ]
  3. Newman-Tancredi A, Rivet JM, Cussac D, Touzard M, Chaput C, Marini L, Millan MJ: Comparison of hippocampal G protein activation by 5-HT(1A) receptor agonists and the atypical antipsychotics clozapine and S16924. Naunyn Schmiedebergs Arch Pharmacol. 2003 Sep;368(3):188-99. Epub 2003 Aug 16. [PubMed:12923612 ]
  4. Zahorodna A, Bobula B, Grzegorzewska M, Tokarski K, Hess G: The influence of repeated administration of clozapine and haloperidol on the effects of the activation of 5-HT(1A), 5-HT(2) and 5-HT(4) receptors in rat frontal cortex. J Physiol Pharmacol. 2004 Jun;55(2):371-9. [PubMed:15213359 ]
  5. Tomic M, Kundakovic M, Butorovic B, Janac B, Andric D, Roglic G, Ignjatovic D, Kostic-Rajacic S: Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4263-6. [PubMed:15261283 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of ...
Gene Name:
HTR1B
Uniprot ID:
P28222
Molecular Weight:
43567.535 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate c...
Gene Name:
HTR1D
Uniprot ID:
P28221
Molecular Weight:
41906.38 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity.
Gene Name:
HTR1E
Uniprot ID:
P28566
Molecular Weight:
41681.57 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modul...
Gene Name:
HTR2C
Uniprot ID:
P28335
Molecular Weight:
51820.705 Da
References
  1. Sodhi MS, Airey DC, Lambert W, Burnet PW, Harrison PJ, Sanders-Bush E: A rapid new assay to detect RNA editing reveals antipsychotic-induced changes in serotonin-2C transcripts. Mol Pharmacol. 2005 Sep;68(3):711-9. Epub 2005 May 25. [PubMed:15917433 ]
  2. Navailles S, De Deurwaerdere P, Spampinato U: Clozapine and haloperidol differentially alter the constitutive activity of central serotonin2C receptors in vivo. Biol Psychiatry. 2006 Mar 15;59(6):568-75. Epub 2005 Sep 22. [PubMed:16182256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Voltage-gated potassium channel activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses in neurons. It is a cation-specific, but otherwise relatively nonselective, ion channel.
Gene Name:
HTR3A
Uniprot ID:
P46098
Molecular Weight:
55279.835 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. It has a high affinity for tricyclic psychotropic drugs (By similarity). Controls pyramidal neurons migration during corticogenesis, through...
Gene Name:
HTR6
Uniprot ID:
P50406
Molecular Weight:
46953.625 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase.
Gene Name:
HTR7
Uniprot ID:
P34969
Molecular Weight:
53554.43 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonist
General Function:
Histamine receptor activity
Specific Function:
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
Molecular Weight:
55783.61 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Roegge CS, Perraut C, Hao X, Levin ED: Histamine H1 receptor involvement in prepulse inhibition and memory function: relevance for the antipsychotic actions of clozapine. Pharmacol Biochem Behav. 2007 Apr;86(4):686-92. Epub 2007 Feb 22. [PubMed:17382376 ]
  3. Leysen JE, Janssen PM, Megens AA, Schotte A: Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry. 1994 May;55 Suppl:5-12. [PubMed:7520908 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonist
General Function:
Histamine receptor activity
Specific Function:
The H4 subclass of histamine receptors could mediate the histamine signals in peripheral tissues. Displays a significant level of constitutive activity (spontaneous activity in the absence of agonist).
Gene Name:
HRH4
Uniprot ID:
Q9H3N8
Molecular Weight:
44495.375 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Sugata Y, Okano M, Fujiwara T, Matsumoto R, Hattori H, Yamamoto M, Nishibori M, Nishizaki K: Histamine H4 receptor agonists have more activities than H4 agonism in antigen-specific human T-cell responses. Immunology. 2007 Jun;121(2):266-75. Epub 2007 Mar 7. [PubMed:17346280 ]
  3. Smits RA, Lim HD, Stegink B, Bakker RA, de Esch IJ, Leurs R: Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives. J Med Chem. 2006 Jul 27;49(15):4512-6. [PubMed:16854056 ]
  4. Adachi N, Liu K, Motoki A, Nishibori M, Arai T: Suppression of ischemia/reperfusion liver injury by histamine H4 receptor stimulation in rats. Eur J Pharmacol. 2006 Aug 21;544(1-3):181-7. Epub 2006 Jun 29. [PubMed:16860312 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1B
Uniprot ID:
P35368
Molecular Weight:
56835.375 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonist
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonist
General Function:
Epinephrine binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
Molecular Weight:
49565.8 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonist
General Function:
Protein homodimerization activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name:
ADRA2C
Uniprot ID:
P18825
Molecular Weight:
49521.585 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonist
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM1
Uniprot ID:
P11229
Molecular Weight:
51420.375 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonist
General Function:
G-protein coupled acetylcholine receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
Molecular Weight:
51714.605 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonist
General Function:
Receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM3
Uniprot ID:
P20309
Molecular Weight:
66127.445 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonist
General Function:
Guanyl-nucleotide exchange factor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is inhibition of adenylate cyclase.
Gene Name:
CHRM4
Uniprot ID:
P08173
Molecular Weight:
53048.65 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
antagonist
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM5
Uniprot ID:
P08912
Molecular Weight:
60073.205 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
unknown
General Function:
Clathrin light chain binding
Specific Function:
Interacts with clathrin light chain A and stimulates clathrin self-assembly and clathrin-mediated endocytosis.
Gene Name:
CALY
Uniprot ID:
Q9NYX4
Molecular Weight:
23433.49 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Brosen K: Drug interactions and the cytochrome P450 system. The role of cytochrome P450 1A2. Clin Pharmacokinet. 1995;29 Suppl 1:20-5. [PubMed:8846619 ]
  2. Wang B, Zhou SF: Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218. [PubMed:19754423 ]
  3. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  4. Fang J, Coutts RT, McKenna KF, Baker GB: Elucidation of individual cytochrome P450 enzymes involved in the metabolism of clozapine. Naunyn Schmiedebergs Arch Pharmacol. 1998 Nov;358(5):592-9. [PubMed:9840430 ]
  5. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  6. Carrillo JA, Benitez J: Clinically significant pharmacokinetic interactions between dietary caffeine and medications. Clin Pharmacokinet. 2000 Aug;39(2):127-53. [PubMed:10976659 ]
  7. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Trimethylamine monooxygenase activity
Specific Function:
Involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. It N-oxygenates primary aliphatic alkylamines as well as secondary and tertiary amines. Plays an important role in the metabolism of trimethylamine (TMA), via the production of TMA N-oxide (TMAO). Is also able to perform S-oxidation when acting on sulfide compounds (PubMed:9224773).
Gene Name:
FMO3
Uniprot ID:
P31513
Molecular Weight:
60032.975 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Protein homodimerization activity
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Isoform 2 lacks transferase activity but acts as a negative regulator of isoform 1 (By similarity).
Gene Name:
UGT1A4
Uniprot ID:
P22310
Molecular Weight:
60024.535 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Vitamin d 24-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, retinoid and xenobiotics. Preferentially oxidizes 17beta-estradiol to the carcinogenic 4-hydroxy derivative, and a variety of procarcinogenic compou...
Gene Name:
CYP1B1
Uniprot ID:
Q16678
Molecular Weight:
60845.33 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Boulton DW, DeVane CL, Liston HL, Markowitz JS: In vitro P-glycoprotein affinity for atypical and conventional antipsychotics. Life Sci. 2002 May 31;71(2):163-9. [PubMed:12031686 ]
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Drug created on June 13, 2005 07:24 / Updated on July 31, 2016 01:52