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Identification
NameThiothixene
Accession NumberDB01623
TypeSmall Molecule
GroupsApproved
Description

A thioxanthine used as an antipsychotic agent. Its effects are similar to the phenothiazine antipsychotics. [PubChem]

Structure
Thumb
Synonyms
(e)-thiothixene
cis-thiothixene
Thiothixine
Tiotixene
Tiotixeno
Tiotixenum
External Identifiers
  • NSC-108165
  • P-4657 B
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Navane Cap 2mgcapsule2 mgoralErfa Canada 2012 Inc1969-12-312015-06-05Canada
Navane Cap 5mgcapsule5 mgoralErfa Canada 2012 Inc1969-12-31Not applicableCanada
Navane Capsules 10mgcapsule10 mgoralErfa Canada 2012 Inc1969-12-312015-06-05Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Thiothixenecapsule5 mg/1oralMylan Institutional Inc.1998-03-05Not applicableUs
Thiothixenecapsule5 mg/1oralRebel Distributors Corp1987-06-24Not applicableUs
Thiothixenecapsule1 mg/1oralMylan Pharmaceuticals Inc.1987-06-23Not applicableUs
Thiothixenecapsule10 mg/1oralMylan Institutional Inc.1998-07-24Not applicableUs
Thiothixenecapsule2 mg/1oralMylan Institutional Inc.1998-03-09Not applicableUs
Thiothixenecapsule10 mg/1oralSandoz Inc1987-06-24Not applicableUs
Thiothixenecapsule5 mg/1oralREMEDYREPACK INC.2011-11-14Not applicableUs
Thiothixenecapsule5 mg/1oralSandoz Inc1987-06-24Not applicableUs
Thiothixenecapsule2 mg/1oralREMEDYREPACK INC.2011-12-07Not applicableUs
Thiothixenecapsule2 mg/1oralSandoz Inc1987-06-24Not applicableUs
Thiothixenecapsule1 mg/1oralREMEDYREPACK INC.2011-10-25Not applicableUs
Thiothixenecapsule1 mg/1oralSandoz Inc1987-06-24Not applicableUs
Thiothixenecapsule2 mg/1oralREMEDYREPACK INC.2011-08-17Not applicableUs
Thiothixenecapsule10 mg/1oralMylan Pharmaceuticals Inc.1987-06-23Not applicableUs
Thiothixenecapsule5 mg/1oralREMEDYREPACK INC.2011-07-22Not applicableUs
Thiothixenecapsule5 mg/1oralMylan Pharmaceuticals Inc.1987-06-23Not applicableUs
Thiothixenecapsule5 mg/1oralCarilion Materials Management1987-06-23Not applicableUs
Thiothixenecapsule10 mg/1oralREMEDYREPACK INC.2011-07-19Not applicableUs
Thiothixenecapsule2 mg/1oralMylan Pharmaceuticals Inc.1987-06-23Not applicableUs
Thiothixenecapsule10 mg/1oralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
NavanNot Available
NavaronNot Available
OrbinamonNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Thiothixene hydrochloride
ThumbNot applicableDBSALT001423
Categories
UNII7318FJ13YJ
CAS number3313-26-6
WeightAverage: 443.625
Monoisotopic: 443.170118567
Chemical FormulaC23H29N3O2S2
InChI KeyInChIKey=GFBKORZTTCHDGY-UWVJOHFNSA-N
InChI
InChI=1S/C23H29N3O2S2/c1-24(2)30(27,28)18-10-11-23-21(17-18)19(20-7-4-5-9-22(20)29-23)8-6-12-26-15-13-25(3)14-16-26/h4-5,7-11,17H,6,12-16H2,1-3H3/b19-8-
IUPAC Name
(9Z)-N,N-dimethyl-9-[3-(4-methylpiperazin-1-yl)propylidene]-9H-thioxanthene-2-sulfonamide
SMILES
CN(C)S(=O)(=O)C1=CC2=C(SC3=CC=CC=C3\C2=C\CCN2CCN(C)CC2)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as thioxanthenes. These are organic polycyclic compounds containing a thioxanthene moiety, which is an aromatic tricycle derived from xanthene by replacing the oxygen atom with a sulfur atom.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzothiopyrans
Sub Class1-benzothiopyrans
Direct ParentThioxanthenes
Alternative Parents
Substituents
  • Thioxanthene
  • Diarylthioether
  • Benzenesulfonamide
  • N-alkylpiperazine
  • N-methylpiperazine
  • Benzenoid
  • Piperazine
  • 1,4-diazinane
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Thioether
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the management of schizophrenia.
PharmacodynamicsThiothixene is an antipsychotic of the thioxanthene series. Navane possesses certain chemical and pharmacological similarities to the piperazine phenothiazines and differences from the aliphatic group of phenothiazines. Although widely used in the treatment of schizophrenia for several decades, thiothixene is seldom used today in favor of atypical antipsychotics such as risperidone.
Mechanism of actionThiothixene acts as an antagonist (blocking agent) on different postsysnaptic receptors -on dopaminergic-receptors (subtypes D1, D2, D3 and D4 - different antipsychotic properties on productive and unproductive symptoms), on serotonergic-receptors (5-HT1 and 5-HT2, with anxiolytic, antidepressive and antiaggressive properties as well as an attenuation of extrapypramidal side-effects, but also leading to weight gain, fall in blood pressure, sedation and ejaculation difficulties), on histaminergic-receptors (H1-receptors, sedation, antiemesis, vertigo, fall in blood pressure and weight gain), alpha1/alpha2-receptors (antisympathomimetic properties, lowering of blood pressure, reflex tachycardia, vertigo, sedation, hypersalivation and incontinence as well as sexual dysfunction, but may also attenuate pseudoparkinsonism - controversial) and finally on muscarinic (cholinergic) M1/M2-receptors (causing anticholinergic symptoms like dry mouth, blurred vision, obstipation, difficulty/inability to urinate, sinus tachycardia, ECG-changes and loss of memory, but the anticholinergic action may attenuate extrapyramidal side-effects).
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic.

Route of eliminationNot Available
Half life10-20 hours
ClearanceNot Available
ToxicitySymptoms of overdose include central nervous system depression, coma, difficulty swallowing, dizziness, drowsiness, head tilted to the side, low blood pressure, muscle twitching, rigid muscles, salivation, tremors, walking disturbances, and weakness.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9969
Blood Brain Barrier+0.9437
Caco-2 permeable-0.6277
P-glycoprotein substrateSubstrate0.8707
P-glycoprotein inhibitor IInhibitor0.9247
P-glycoprotein inhibitor IIInhibitor0.9036
Renal organic cation transporterNon-inhibitor0.5373
CYP450 2C9 substrateNon-substrate0.7951
CYP450 2D6 substrateNon-substrate0.9117
CYP450 3A4 substrateSubstrate0.5269
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorInhibitor0.8933
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorInhibitor0.796
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5406
Ames testNon AMES toxic0.651
CarcinogenicityNon-carcinogens0.8173
BiodegradationNot ready biodegradable0.947
Rat acute toxicity2.7586 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5093
hERG inhibition (predictor II)Non-inhibitor0.7259
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Capsuleoral2 mg
Capsuleoral5 mg
Capsuleoral10 mg
Capsuleoral1 mg/1
Capsuleoral10 mg/1
Capsuleoral2 mg/1
Capsuleoral5 mg/1
Prices
Unit descriptionCostUnit
Navane 20 mg capsule3.15USD capsule
Navane 10 mg capsule1.66USD capsule
Navane 5 mg capsule1.2USD capsule
Navane 2 mg capsule0.8USD capsule
Thiothixene 10 mg capsule0.67USD capsule
Thiothixene 5 mg capsule0.47USD capsule
Thiothixene 2 mg capsule0.31USD capsule
Thiothixene 1 mg capsule0.24USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0139 mg/mLALOGPS
logP4.01ALOGPS
logP3.36ChemAxon
logS-4.5ALOGPS
pKa (Strongest Basic)8.56ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area43.86 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity137.85 m3·mol-1ChemAxon
Polarizability50.35 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesN05AF04
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Thiothixene can be increased when it is combined with Abiraterone.
AclidiniumAclidinium may increase the anticholinergic activities of Thiothixene.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Thiothixene.
AmisulprideThe risk or severity of adverse effects can be increased when Thiothixene is combined with Amisulpride.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Thiothixene.
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Thiothixene.
AmphetamineThiothixene may decrease the stimulatory activities of Amphetamine.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Thiothixene.
AzelastineThiothixene 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 Thiothixene.
BenzphetamineThiothixene may decrease the stimulatory activities of Benzphetamine.
BortezomibThe metabolism of Thiothixene can be decreased when combined with Bortezomib.
Botulinum Toxin Type AThiothixene may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BThiothixene may increase the anticholinergic activities of Botulinum Toxin Type B.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Thiothixene.
BromocriptineThe therapeutic efficacy of Thiothixene can be decreased when used in combination with Bromocriptine.
BuprenorphineThiothixene 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 Thiothixene.
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Thiothixene.
CarbamazepineThe metabolism of Thiothixene can be increased when combined with Carbamazepine.
CathinoneThiothixene may decrease the stimulatory activities of Cathinone.
Cimetropium BromideThiothixene may increase the anticholinergic activities of Cimetropium Bromide.
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Thiothixene.
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Thiothixene.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Thiothixene.
Cyproterone acetateThe serum concentration of Thiothixene can be decreased when it is combined with Cyproterone acetate.
DeferasiroxThe serum concentration of Thiothixene can be increased when it is combined with Deferasirox.
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Thiothixene.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Desvenlafaxine is combined with Thiothixene.
DextroamphetamineThiothixene may decrease the stimulatory activities of Dextroamphetamine.
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Thiothixene.
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Thiothixene.
DofetilideThiothixene may increase the QTc-prolonging activities of Dofetilide.
DonepezilDonepezil may increase the central neurotoxic activities of Thiothixene.
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Thiothixene.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Thiothixene.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Thiothixene.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Thiothixene.
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Thiothixene.
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Thiothixene.
EluxadolineThiothixene may increase the activities of Eluxadoline.
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Thiothixene.
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Thiothixene.
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Thiothixene.
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Thiothixene.
EthanolThiothixene may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Thiothixene.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Thiothixene.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Thiothixene.
FrovatriptanThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Thiothixene.
GalantamineGalantamine may increase the central neurotoxic activities of Thiothixene.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Thiothixene is combined with Glucagon recombinant.
GoserelinThiothixene may increase the QTc-prolonging activities of Goserelin.
HydrocodoneThiothixene may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Thiothixene.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Thiothixene.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Thiothixene.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Thiothixene.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Thiothixene.
LeuprolideThiothixene may increase the QTc-prolonging activities of Leuprolide.
LevomilnacipranThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Thiothixene.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Thiothixene.
LisdexamfetamineThiothixene may decrease the stimulatory activities of Lisdexamfetamine.
LithiumLithium may increase the neurotoxic activities of Thiothixene.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Thiothixene.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Thiothixene.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Thiothixene.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Thiothixene.
MequitazineThiothixene may increase the arrhythmogenic activities of Mequitazine.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Thiothixene.
MethamphetamineThiothixene may decrease the stimulatory activities of Methamphetamine.
MethotrimeprazineThiothixene may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethylphenidateThe risk or severity of adverse effects can be increased when Thiothixene is combined with Methylphenidate.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Thiothixene.
MetyrosineThiothixene may increase the sedative activities of Metyrosine.
MexiletineThe metabolism of Thiothixene can be decreased when combined with Mexiletine.
MianserinMianserin may increase the anticholinergic activities of Thiothixene.
MifepristoneMifepristone may increase the QTc-prolonging activities of Thiothixene.
MilnacipranThe risk or severity of adverse effects can be increased when Milnacipran is combined with Thiothixene.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Thiothixene.
MirabegronThe risk or severity of adverse effects can be increased when Thiothixene is combined with Mirabegron.
MirtazapineThiothixene may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Thiothixene.
MorphineThe risk or severity of adverse effects can be increased when Thiothixene is combined with Morphine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Thiothixene.
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Thiothixene.
NefazodoneThe risk or severity of adverse effects can be increased when Nefazodone is combined with Thiothixene.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Thiothixene.
OrphenadrineThiothixene may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeThiothixene may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Thiothixene is combined with Paroxetine.
Peginterferon alfa-2bThe serum concentration of Thiothixene can be increased when it is combined with Peginterferon alfa-2b.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Thiothixene.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Thiothixene.
PhendimetrazineThiothixene may decrease the stimulatory activities of Phendimetrazine.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Thiothixene.
PhentermineThiothixene may decrease the stimulatory activities of Phentermine.
Potassium ChlorideThiothixene may increase the ulcerogenic activities of Potassium Chloride.
PramlintidePramlintide may increase the anticholinergic activities of Thiothixene.
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Thiothixene.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Thiothixene.
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Thiothixene.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Thiothixene.
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Thiothixene.
RamosetronThiothixene may increase the activities of Ramosetron.
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Thiothixene.
RivastigmineRivastigmine may increase the central neurotoxic activities of Thiothixene.
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Thiothixene.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Thiothixene.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Thiothixene.
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Thiothixene.
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Thiothixene.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Thiothixene.
SulpirideThe risk or severity of adverse effects can be increased when Thiothixene is combined with Sulpiride.
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Thiothixene.
SuvorexantThiothixene may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineThe therapeutic efficacy of Thiothixene can be decreased when used in combination with Tacrine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Thiothixene.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Thiothixene.
TeriflunomideThe serum concentration of Thiothixene can be decreased when it is combined with Teriflunomide.
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Thiothixene.
ThalidomideThiothixene may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TiotropiumThiothixene may increase the anticholinergic activities of Tiotropium.
TopiramateThe risk or severity of adverse effects can be increased when Thiothixene is combined with Topiramate.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Thiothixene.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Thiothixene.
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Thiothixene.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Thiothixene.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Thiothixene.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Thiothixene.
VemurafenibThe serum concentration of Thiothixene can be increased when it is combined with Vemurafenib.
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Thiothixene.
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Thiothixene.
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Thiothixene.
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Thiothixene.
ZolpidemThiothixene may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Avoid alcohol

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. Shultz PJ, Sedor JR, Abboud HE: Dopaminergic stimulation of cAMP accumulation in cultured rat mesangial cells. Am J Physiol. 1987 Aug;253(2 Pt 2):H358-64. [PubMed:3039860 ]
  2. Oades RD, Rao ML, Bender S, Sartory G, Muller BW: Neuropsychological and conditioned blocking performance in patients with schizophrenia: assessment of the contribution of neuroleptic dose, serum levels and dopamine D2-receptor occupancy. Behav Pharmacol. 2000 Jun;11(3-4):317-30. [PubMed:11103886 ]
  3. Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [PubMed:11873706 ]
  4. Wu S, Xing Q, Gao R, Li X, Gu N, Feng G, He L: Response to chlorpromazine treatment may be associated with polymorphisms of the DRD2 gene in Chinese schizophrenic patients. Neurosci Lett. 2005 Mar 7;376(1):1-4. Epub 2004 Dec 2. [PubMed:15694263 ]
  5. Wu SN, Gao R, Xing QH, Li HF, Shen YF, Gu NF, Feng GY, He L: Association of DRD2 polymorphisms and chlorpromazine-induced extrapyramidal syndrome in Chinese schizophrenic patients. Acta Pharmacol Sin. 2006 Aug;27(8):966-70. [PubMed:16867246 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  7. Seeman P: Dopamine D2 receptors as treatment targets in schizophrenia. Clin Schizophr Relat Psychoses. 2010 Apr;4(1):56-73. doi: 10.3371/CSRP.4.1.5. [PubMed:20643630 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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. Shultz PJ, Sedor JR, Abboud HE: Dopaminergic stimulation of cAMP accumulation in cultured rat mesangial cells. Am J Physiol. 1987 Aug;253(2 Pt 2):H358-64. [PubMed:3039860 ]
  2. Kanba S, Suzuki E, Nomura S, Nakaki T, Yagi G, Asai M, Richelson E: Affinity of neuroleptics for D1 receptor of human brain striatum. J Psychiatry Neurosci. 1994 Jul;19(4):265-9. [PubMed:7918347 ]
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. Kusumi I, Takahashi Y, Suzuki K, Kameda K, Koyama T: Differential effects of subchronic treatments with atypical antipsychotic drugs on dopamine D2 and serotonin 5-HT2A receptors in the rat brain. J Neural Transm (Vienna). 2000;107(3):295-302. [PubMed:10821438 ]
  2. Yamada J, Sugimoto Y, Horisaka K: Serotonin2 (5-HT2) receptor agonist 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) inhibits chlorpromazine- and haloperidol-induced hypothermia in mice. Biol Pharm Bull. 1995 Nov;18(11):1580-3. [PubMed:8593484 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. 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
inhibitor
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. 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 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
References
  1. Kitamura K, Omran AA, Nagata C, Kamijima Y, Tanaka R, Takegami S, Kitade T: Effects of inorganic ions on the binding of triflupromazine and chlorpromazine to bovine serum albumin studied by spectrometric methods. Chem Pharm Bull (Tokyo). 2006 Jul;54(7):972-6. [PubMed:16819214 ]
  2. Rukhadze MD, Bezarashvili GS, Sidamonidze NS, Tsagareli SK: Investigation of binding process of chlorpromazine to bovine serum albumin by means of passive and active experiments. Biomed Chromatogr. 2001 Oct;15(6):365-73. [PubMed:11559920 ]
  3. Silva D, Cortez CM, Louro SR: Quenching of the intrinsic fluorescence of bovine serum albumin by chlorpromazine and hemin. Braz J Med Biol Res. 2004 Jul;37(7):963-8. Epub 2004 Jun 22. [PubMed:15264002 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Secondary active organic cation transmembrane transporter activity
Specific Function:
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. Bednarczyk D, Ekins S, Wikel JH, Wright SH: Influence of molecular structure on substrate binding to the human organic cation transporter, hOCT1. Mol Pharmacol. 2003 Mar;63(3):489-98. [PubMed:12606755 ]
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Drug created on August 29, 2007 14:17 / Updated on May 01, 2016 13:40