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Identification
NameLoxapine
Accession NumberDB00408  (APRD00574)
TypeSmall Molecule
GroupsApproved
Description

An antipsychotic agent used in schizophrenia. [PubChem]

Structure
Thumb
Synonyms
2-Chloro-11-(4-methyl-1-piperazinyl)dibenz[b,f][1,4]oxazepine
Cloxazepine
Loxapina
Loxapine
Loxapinum
oxilapine
External Identifiers
  • AZ-004
  • BRN 0626753
  • CL 62362
  • CL 71563
  • HF 3170
  • LW 3170
  • S 805
  • SUM 3170
  • UNII-376MYL4MAL
  • UNII-LER583670J
  • UNII-X59SG0MRYU
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Adasuveaerosol, powder10 mg/1respiratory (inhalation)Teva Select Brands2014-01-22Not applicableUs
Dom-loxapine Tablets 10mgtablet10 mgoralDominion Pharmacal1999-09-15Not applicableCanada
Dom-loxapine Tablets 25mgtablet25 mgoralDominion Pharmacal1999-09-15Not applicableCanada
Dom-loxapine Tablets 50mgtablet50 mgoralDominion Pharmacal1999-09-15Not applicableCanada
Dom-loxapine Tablets 5mgtablet5 mgoralDominion Pharmacal1999-09-15Not applicableCanada
Loxapac - Tab 10mgtablet10 mgoralWyeth Ayerst Canada Inc.1997-09-242002-02-06Canada
Loxapac - Tab 50mgtablet50 mgoralWyeth Ayerst Canada Inc.1997-02-042001-05-22Canada
Loxapac - Tab 5mgtablet5 mgoralWyeth Ayerst Canada Inc.1997-02-042002-07-31Canada
Loxapac Imliquid50 mgintramuscularSandoz Canada Incorporated1997-06-13Not applicableCanada
Loxapac Inj 50mg/mlliquid50 mgintramuscularLederle Cyanamid Canada Inc.1980-12-311997-08-14Canada
Loxapac Oral Concentrate-liq 25mg/mlliquid25 mgoralWyeth Ayerst Canada Inc.1996-11-152001-09-19Canada
Loxapac Orl Conc 25mg/mlliquid25 mgoralLederle Cyanamid Canada Inc.1976-12-311997-08-14Canada
Loxapac Tab 10mgtablet13.6 mgoralLederle Cyanamid Canada Inc.1975-12-311999-04-12Canada
Loxapac Tab 25mgtablet34 mgoralLederle Cyanamid Canada Inc.1975-12-311997-08-14Canada
Loxapac Tab 50mgtablet68 mgoralLederle Cyanamid Canada Inc.1976-12-311997-08-14Canada
Loxapac Tab 5mgtablet6.8 mgoralLederle Cyanamid Canada Inc.1976-12-311997-08-14Canada
Loxapac Tablets - 25 mgtablet25 mgoralWyeth Ayerst Canada Inc.1997-06-132002-03-19Canada
Loxapine Hydrochloride Im Injection 50mg/mlliquid50 mgintramuscularWy Pharma Inc.Not applicableNot applicableCanada
Loxapine Hydrochloride Oral Concentrate 25mg/mlliquid25 mgoralWy Pharma Inc.Not applicableNot applicableCanada
Loxapine Succinate Tablets 10mgtablet10 mgoralWy Pharma Inc.Not applicableNot applicableCanada
Loxapine Succinate Tablets 25mgtablet25 mgoralWy Pharma Inc.Not applicableNot applicableCanada
Loxapine Succinate Tablets 5 mgtablet5 mgoralWy Pharma Inc.Not applicableNot applicableCanada
Loxapine Succinate Tablets 50mgtablet50 mgoralWy Pharma Inc.Not applicableNot applicableCanada
Loxapine-10tablet10 mgoralPro Doc Limitee1998-09-012010-07-13Canada
Loxapine-25tablet25 mgoralPro Doc Limitee1998-09-012010-07-13Canada
Loxapine-5tablet5 mgoralPro Doc Limitee1998-09-012010-07-13Canada
Loxapine-50tablet50 mgoralPro Doc Limitee1998-09-012010-07-13Canada
Nu-loxapinetablet10 mgoralNu Pharm Inc1998-07-022012-09-04Canada
Nu-loxapinetablet50 mgoralNu Pharm Inc1998-07-132012-09-04Canada
Nu-loxapinetablet5 mgoralNu Pharm Inc1998-07-022012-09-04Canada
Nu-loxapinetablet25 mgoralNu Pharm Inc1998-07-062012-09-04Canada
PHL-loxapinetablet5 mgoralPharmel Inc1998-02-16Not applicableCanada
PHL-loxapinetablet50 mgoralPharmel Inc1998-02-16Not applicableCanada
PHL-loxapinesolution25 mgoralPharmel Inc2004-07-22Not applicableCanada
PHL-loxapinetablet25 mgoralPharmel Inc1998-02-16Not applicableCanada
PHL-loxapinetablet2.5 mgoralPharmel Inc2004-07-22Not applicableCanada
PHL-loxapinetablet10 mgoralPharmel Inc1998-02-16Not applicableCanada
Xylactablet2.5 mgoralPendopharm Division Of De Pharmascience Inc2000-10-05Not applicableCanada
Xylactablet50 mgoralPendopharm Division Of De Pharmascience Inc1998-04-16Not applicableCanada
Xylactablet25 mgoralPendopharm Division Of De Pharmascience Inc1997-07-08Not applicableCanada
Xylacsolution25 mgoralPendopharm Division Of De Pharmascience Inc1998-12-03Not applicableCanada
Xylactablet10 mgoralPendopharm Division Of De Pharmascience Inc1998-04-16Not applicableCanada
Xylactablet5 mgoralPendopharm Division Of De Pharmascience Inc1997-06-13Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-loxapinetablet50 mgoralApotex Inc1998-03-30Not applicableCanada
Apo-loxapinetablet25 mgoralApotex Inc1998-03-30Not applicableCanada
Apo-loxapinetablet10 mgoralApotex Inc1998-03-30Not applicableCanada
Apo-loxapinetablet5 mgoralApotex Inc1998-03-30Not applicableCanada
Loxapinetablet10 mg/1oralMarlex Pharmaceuticals Inc2014-10-01Not applicableUs
Loxapinecapsule10 mg/1oralEpic Pharma, LLC2015-01-02Not applicableUs
Loxapinetablet50 mg/1oralMarlex Pharmaceuticals Inc2014-10-01Not applicableUs
Loxapinecapsule5 mg/1oralMylan Pharmaceuticals Inc.2004-11-03Not applicableUs
Loxapinecapsule50 mg/1oralEpic Pharma, LLC2015-01-02Not applicableUs
Loxapinecapsule5 mg/1oralClinical Solutions Wholesale1988-06-15Not applicableUs
Loxapinecapsule50 mg/1oralAmerican Health Packaging2013-06-24Not applicableUs
Loxapinecapsule25 mg/1oralLannett Company, Inc.2011-09-26Not applicableUs
Loxapinecapsule5 mg/1oralEpic Pharma, LLC2015-01-02Not applicableUs
Loxapinetablet5 mg/1oralMarlex Pharmaceuticals Inc2014-10-01Not applicableUs
Loxapinecapsule25 mg/1oralAmerican Health Packaging2013-06-24Not applicableUs
Loxapinecapsule10 mg/1oralLannett Company, Inc.2011-09-26Not applicableUs
Loxapinecapsule50 mg/1oralWatson Laboratories, Inc.1988-06-15Not applicableUs
Loxapinecapsule5 mg/1oralLannett Company, Inc.2011-09-26Not applicableUs
Loxapinecapsule10 mg/1oralAmerican Health Packaging2013-06-24Not applicableUs
Loxapinecapsule25 mg/1oralWatson Laboratories, Inc.1988-06-15Not applicableUs
Loxapinecapsule10 mg/1oralREMEDYREPACK INC.2014-05-21Not applicableUs
Loxapinecapsule50 mg/1oralMylan Pharmaceuticals Inc.2004-11-03Not applicableUs
Loxapinecapsule50 mg/1oralClinical Solutions Wholesale1988-06-15Not applicableUs
Loxapinecapsule10 mg/1oralWatson Laboratories, Inc.1988-06-15Not applicableUs
Loxapinecapsule50 mg/1oralMylan Institutional Inc.2004-12-15Not applicableUs
Loxapinecapsule25 mg/1oralMylan Pharmaceuticals Inc.2004-11-03Not applicableUs
Loxapinecapsule25 mg/1oralClinical Solutions Wholesale1988-06-15Not applicableUs
Loxapinecapsule5 mg/1oralWatson Laboratories, Inc.1988-06-15Not applicableUs
Loxapinecapsule25 mg/1oralMylan Institutional Inc.2004-12-15Not applicableUs
Loxapinetablet25 mg/1oralMarlex Pharmaceuticals Inc2014-10-01Not applicableUs
Loxapinecapsule25 mg/1oralEpic Pharma, LLC2015-01-02Not applicableUs
Loxapinecapsule10 mg/1oralMylan Pharmaceuticals Inc.2004-11-03Not applicableUs
Loxapinecapsule10 mg/1oralClinical Solutions Wholesale1988-06-15Not applicableUs
Loxapinecapsule50 mg/1oralLannett Company, Inc.2011-09-26Not applicableUs
Loxapinecapsule10 mg/1oralMylan Institutional Inc.2004-12-15Not applicableUs
Loxapinecapsule5 mg/1oralCarilion Materials Management1988-06-15Not applicableUs
Loxapine Succinatecapsule50 mg/1oralREMEDYREPACK INC.2011-09-15Not applicableUs
Loxapine Succinatecapsule5 mg/1oralREMEDYREPACK INC.2011-09-15Not applicableUs
Loxapine Succinatecapsule25 mg/1oralREMEDYREPACK INC.2011-08-15Not applicableUs
Loxapine Succinatecapsule50 mg/1oralREMEDYREPACK INC.2011-04-26Not applicableUs
Loxapine Succinatecapsule10 mg/1oralREMEDYREPACK INC.2010-12-08Not applicableUs
Loxapine Succinatecapsule5 mg/1oralREMEDYREPACK INC.2010-11-30Not applicableUs
Loxitanecapsule25 mg/1oralWatson Pharma, Inc.1988-06-15Not applicableUs
Loxitanecapsule10 mg/1oralWatson Pharma, Inc.1988-06-15Not applicableUs
Loxitanecapsule5 mg/1oralWatson Pharma, Inc.1988-06-15Not applicableUs
Loxitanecapsule50 mg/1oralWatson Pharma, Inc.1988-06-15Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
CloxazepineNot Available
LopacNewai Chem
LosagenPatron
LoxapacWyeth
RosupSwiss Pharm
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Loxapine hydrochloride
ThumbNot applicableDBSALT001429
Loxapine succinate
ThumbNot applicableDBSALT001194
Categories
UNIILER583670J
CAS number1977-10-2
WeightAverage: 327.808
Monoisotopic: 327.11383992
Chemical FormulaC18H18ClN3O
InChI KeyInChIKey=XJGVXQDUIWGIRW-UHFFFAOYSA-N
InChI
InChI=1S/C18H18ClN3O/c1-21-8-10-22(11-9-21)18-14-12-13(19)6-7-16(14)23-17-5-3-2-4-15(17)20-18/h2-7,12H,8-11H2,1H3
IUPAC Name
13-chloro-10-(4-methylpiperazin-1-yl)-2-oxa-9-azatricyclo[9.4.0.0³,⁸]pentadeca-1(11),3,5,7,9,12,14-heptaene
SMILES
CN1CCN(CC1)C1=NC2=CC=CC=C2OC2=C1C=C(Cl)C=C2
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as dibenzoxazepines. These are compounds containing a dibenzoxazepine moiety, which consists of two benzene connected by an oxazepine ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzoxazepines
Sub ClassDibenzoxazepines
Direct ParentDibenzoxazepines
Alternative Parents
Substituents
  • Dibenzoxazepine
  • Diaryl ether
  • N-alkylpiperazine
  • N-methylpiperazine
  • Chlorobenzene
  • Imidolactam
  • Benzenoid
  • Piperazine
  • 1,4-diazinane
  • Aryl halide
  • Aryl chloride
  • Tertiary aliphatic amine
  • Tertiary amine
  • Oxacycle
  • Azacycle
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Ether
  • Carboxylic acid amidine
  • Amidine
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the management of the manifestations of psychotic disorders such as schizophrenia
PharmacodynamicsLoxapine, a dibenzoxazepine compound, represents a subclass of tricyclic antipsychotic agents, chemically distinct from the thioxanthenes, butyrophenones, and phenothiazines. Pharmacologically, Loxapine is a tranquilizer for which the exact mode of action has not been established, however, it is believed that by antagonising dopamine and serotonin receptors, there is a marked cortical inhibition which can manifest as tranquilization and suppression of aggression.
Mechanism of actionLoxapine is a dopamine antagonist, and also a serotonin 5-HT2 blocker. The exact mode of action of Loxapine has not been established, however changes in the level of excitability of subcortical inhibitory areas have been observed in several animal species in association with such manifestations of tranquilization as calming effects and suppression of aggressive behavior.
Related Articles
AbsorptionSystemic bioavailability of the parent drug was only about one third that after an equivalent intramuscular dose (25 mg base) in male volunteers
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic

Route of eliminationMetabolites are excreted in the urine in the form of conjugates and in the feces unconjugated.
Half lifeOral-4 hours
ClearanceNot Available
ToxicityLD50=65 mg/kg (Orally in mice)
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+0.9944
Blood Brain Barrier+0.9801
Caco-2 permeable+0.5531
P-glycoprotein substrateSubstrate0.8545
P-glycoprotein inhibitor IInhibitor0.8525
P-glycoprotein inhibitor IIInhibitor0.8388
Renal organic cation transporterInhibitor0.7084
CYP450 2C9 substrateNon-substrate0.7331
CYP450 2D6 substrateSubstrate0.7155
CYP450 3A4 substrateSubstrate0.6309
CYP450 1A2 substrateInhibitor0.8159
CYP450 2C9 inhibitorNon-inhibitor0.8755
CYP450 2D6 inhibitorInhibitor0.7543
CYP450 2C19 inhibitorNon-inhibitor0.6217
CYP450 3A4 inhibitorNon-inhibitor0.9393
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6968
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.8743
BiodegradationNot ready biodegradable1.0
Rat acute toxicity3.3057 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.5701
hERG inhibition (predictor II)Inhibitor0.6141
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Watson laboratories inc
  • Actavis totowa llc
  • Mylan pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Aerosol, powderrespiratory (inhalation)10 mg/1
Liquidintramuscular50 mg
Liquidoral25 mg
Tabletoral13.6 mg
Tabletoral34 mg
Tabletoral68 mg
Tabletoral6.8 mg
Capsuleoral10 mg/1
Capsuleoral25 mg/1
Capsuleoral5 mg/1
Capsuleoral50 mg/1
Tabletoral10 mg/1
Tabletoral25 mg/1
Tabletoral5 mg/1
Tabletoral50 mg/1
Solutionoral25 mg
Tabletoral10 mg
Tabletoral2.5 mg
Tabletoral25 mg
Tabletoral5 mg
Tabletoral50 mg
Prices
Unit descriptionCostUnit
Loxapac 50 mg/ml7.05USD ml
Loxitane 50 mg capsule4.04USD capsule
Loxitane 25 mg capsule3.09USD capsule
Loxapine 50 mg capsule2.57USD capsule
Loxitane 10 mg capsule2.04USD capsule
Loxapine 25 mg capsule1.92USD capsule
Loxitane 5 mg capsule1.58USD capsule
Loxapine 10 mg capsule1.27USD capsule
Loxapine Succinate 5 mg capsule1.03USD capsule
Loxapine 5 mg capsule0.99USD capsule
Pms-Loxapine 50 mg Tablet0.54USD tablet
Pms-Loxapine 25 mg Tablet0.41USD tablet
Pms-Loxapine 10 mg Tablet0.26USD tablet
Pms-Loxapine 5 mg Tablet0.16USD tablet
Pms-Loxapine 2.5 mg Tablet0.08USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6716416 No2002-05-202022-05-20Us
US7052679 No2001-10-262021-10-26Us
US7078020 No2001-10-262021-10-26Us
US7090830 No2001-10-262021-10-26Us
US7458374 No2004-08-182024-08-18Us
US7537009 No2004-10-282024-10-28Us
US7585493 No2001-10-262021-10-26Us
US7601337 No2001-10-262021-10-26Us
US8074644 No2002-07-252022-07-25Us
US8173107 No2001-10-262021-10-26Us
US8235037 No2001-10-262021-10-26Us
US8387612 No2006-10-232026-10-23Us
US8955512 No2001-10-262021-10-26Us
US8991387 No2004-05-212024-05-21Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point109-111 °CU.S. Patents 3,412,193; 3,546,226.
logP3.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.103 mg/mLALOGPS
logP3.18ALOGPS
logP3.46ChemAxon
logS-3.5ALOGPS
pKa (Strongest Basic)7.18ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area28.07 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity95.11 m3·mol-1ChemAxon
Polarizability34.99 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
MSMass Spectrum (Electron Ionization)splash10-0a4l-7590000000-118f30ca0699bf2b3d2eView in MoNA
References
Synthesis Reference

U.S. Patents 3,412,193; 3,546,226.

US3412193
General References
  1. Glazer WM: Does loxapine have "atypical" properties? Clinical evidence. J Clin Psychiatry. 1999;60 Suppl 10:42-6. [PubMed:10340686 ]
  2. Cheung SW, Tang SW, Remington G: Simultaneous quantitation of loxapine, amoxapine and their 7- and 8-hydroxy metabolites in plasma by high-performance liquid chromatography. J Chromatogr. 1991 Mar 8;564(1):213-21. [PubMed:1860915 ]
External Links
ATC CodesN05AH01
AHFS Codes
  • 28:16.08.92
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AclidiniumAclidinium may increase the anticholinergic activities of Loxapine.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Loxapine.
AmantadineThe therapeutic efficacy of Loxapine can be decreased when used in combination with Amantadine.
AmisulprideThe risk or severity of adverse effects can be increased when Loxapine is combined with Amisulpride.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Loxapine.
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Loxapine.
AmphetamineLoxapine may decrease the stimulatory activities of Amphetamine.
ApomorphineThe therapeutic efficacy of Loxapine can be decreased when used in combination with Apomorphine.
ArformoterolThe risk or severity of adverse effects can be increased when Arformoterol is combined with Loxapine.
AzelastineLoxapine 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 Loxapine.
BenzphetamineLoxapine may decrease the stimulatory activities of Benzphetamine.
Botulinum Toxin Type ALoxapine may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BLoxapine may increase the anticholinergic activities of Botulinum Toxin Type B.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Loxapine.
BromocriptineThe therapeutic efficacy of Loxapine can be decreased when used in combination with Bromocriptine.
BudesonideThe risk or severity of adverse effects can be increased when Budesonide is combined with Loxapine.
BuprenorphineLoxapine 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 Loxapine.
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Loxapine.
CarbamazepineThe serum concentration of the active metabolites of Carbamazepine can be increased when Carbamazepine is used in combination with Loxapine.
CarbidopaThe therapeutic efficacy of Loxapine can be decreased when used in combination with Carbidopa.
CathinoneLoxapine may decrease the stimulatory activities of Cathinone.
Cimetropium BromideLoxapine may increase the anticholinergic activities of Cimetropium Bromide.
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Loxapine.
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Loxapine.
Cromoglicic acidThe risk or severity of adverse effects can be increased when Cromoglicic acid is combined with Loxapine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Loxapine.
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Loxapine.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Desvenlafaxine is combined with Loxapine.
DextroamphetamineLoxapine may decrease the stimulatory activities of Dextroamphetamine.
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Loxapine.
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Loxapine.
DonepezilDonepezil may increase the central neurotoxic activities of Loxapine.
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Loxapine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Loxapine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Loxapine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Loxapine.
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Loxapine.
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Loxapine.
EluxadolineLoxapine may increase the activities of Eluxadoline.
EntacaponeThe therapeutic efficacy of Loxapine can be decreased when used in combination with Entacapone.
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Loxapine.
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Loxapine.
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Loxapine.
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Loxapine.
EthanolLoxapine 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 Loxapine.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Loxapine.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Loxapine.
FormoterolThe risk or severity of adverse effects can be increased when Formoterol is combined with Loxapine.
FrovatriptanThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Loxapine.
GalantamineGalantamine may increase the central neurotoxic activities of Loxapine.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Loxapine is combined with Glucagon recombinant.
HydrocodoneLoxapine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Loxapine.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Loxapine.
IndacaterolThe risk or severity of adverse effects can be increased when Indacaterol is combined with Loxapine.
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Loxapine.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Loxapine.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Loxapine.
LevodopaThe therapeutic efficacy of Loxapine can be decreased when used in combination with Levodopa.
LevomilnacipranThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Loxapine.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Loxapine.
LisdexamfetamineLoxapine may decrease the stimulatory activities of Lisdexamfetamine.
LithiumLithium may increase the neurotoxic activities of Loxapine.
LorazepamThe risk or severity of adverse effects can be increased when Loxapine is combined with Lorazepam.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Loxapine.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Loxapine.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Loxapine.
MequitazineLoxapine may increase the arrhythmogenic activities of Mequitazine.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Loxapine.
MethamphetamineLoxapine may decrease the stimulatory activities of Methamphetamine.
MethotrimeprazineLoxapine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethylphenidateThe risk or severity of adverse effects can be increased when Loxapine is combined with Methylphenidate.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Loxapine.
MetyrosineLoxapine may increase the sedative activities of Metyrosine.
MianserinMianserin may increase the anticholinergic activities of Loxapine.
MilnacipranThe risk or severity of adverse effects can be increased when Milnacipran is combined with Loxapine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Loxapine.
MirabegronThe risk or severity of adverse effects can be increased when Loxapine is combined with Mirabegron.
MirtazapineLoxapine 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 Loxapine.
MometasoneThe risk or severity of adverse effects can be increased when Mometasone is combined with Loxapine.
MontelukastThe risk or severity of adverse effects can be increased when Montelukast is combined with Loxapine.
MorphineThe risk or severity of adverse effects can be increased when Loxapine is combined with Morphine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Loxapine.
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Loxapine.
NefazodoneThe risk or severity of adverse effects can be increased when Nefazodone is combined with Loxapine.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Loxapine.
OlodaterolThe risk or severity of adverse effects can be increased when Olodaterol is combined with Loxapine.
OmalizumabThe risk or severity of adverse effects can be increased when Omalizumab is combined with Loxapine.
OrphenadrineLoxapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeLoxapine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Loxapine is combined with Paroxetine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Loxapine.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Loxapine.
PhendimetrazineLoxapine may decrease the stimulatory activities of Phendimetrazine.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Loxapine.
PhentermineLoxapine may decrease the stimulatory activities of Phentermine.
PirbuterolThe risk or severity of adverse effects can be increased when Pirbuterol is combined with Loxapine.
Potassium ChlorideLoxapine may increase the ulcerogenic activities of Potassium Chloride.
PramipexoleThe therapeutic efficacy of Loxapine can be decreased when used in combination with Pramipexole.
PramlintidePramlintide may increase the anticholinergic activities of Loxapine.
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Loxapine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Loxapine.
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Loxapine.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Loxapine.
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Loxapine.
RamosetronLoxapine may increase the activities of Ramosetron.
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Loxapine.
RivastigmineRivastigmine may increase the central neurotoxic activities of Loxapine.
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Loxapine.
RoflumilastThe risk or severity of adverse effects can be increased when Roflumilast is combined with Loxapine.
RopiniroleThe therapeutic efficacy of Loxapine can be decreased when used in combination with Ropinirole.
RotigotineThe therapeutic efficacy of Loxapine can be decreased when used in combination with Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Loxapine.
SalbutamolThe risk or severity of adverse effects can be increased when Salbutamol is combined with Loxapine.
SalmeterolThe risk or severity of adverse effects can be increased when Salmeterol is combined with Loxapine.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Loxapine.
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Loxapine.
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Loxapine.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Loxapine.
SulpirideThe risk or severity of adverse effects can be increased when Loxapine is combined with Sulpiride.
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Loxapine.
SuvorexantLoxapine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineThe therapeutic efficacy of Loxapine can be decreased when used in combination with Tacrine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Loxapine.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Loxapine.
TerbutalineThe risk or severity of adverse effects can be increased when Terbutaline is combined with Loxapine.
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Loxapine.
ThalidomideLoxapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TiotropiumLoxapine may increase the anticholinergic activities of Tiotropium.
TopiramateThe risk or severity of adverse effects can be increased when Loxapine is combined with Topiramate.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Loxapine.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Loxapine.
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Loxapine.
TriamcinoloneThe risk or severity of adverse effects can be increased when Triamcinolone is combined with Loxapine.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Loxapine.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Loxapine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Loxapine.
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Loxapine.
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Loxapine.
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Loxapine.
ZafirlukastThe risk or severity of adverse effects can be increased when Zafirlukast is combined with Loxapine.
ZileutonThe risk or severity of adverse effects can be increased when Zileuton is combined with Loxapine.
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Loxapine.
ZolpidemLoxapine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Take with food to reduce irritation. Avoid alcohol.

Targets

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
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. Lee T, Tang SW: Loxapine and clozapine decrease serotonin (S2) but do not elevate dopamine (D2) receptor numbers in the rat brain. Psychiatry Res. 1984 Aug;12(4):277-85. [PubMed:6239298 ]
  2. Hjerde E, Dahl SG, Sylte I: Atypical and typical antipsychotic drug interactions with the dopamine D2 receptor. Eur J Med Chem. 2005 Feb;40(2):185-94. [PubMed:15694653 ]
  3. Kalkman HO, Neumann V, Nozulak J, Tricklebank MD: Cataleptogenic effect of subtype selective 5-HT receptor antagonists in the rat. Eur J Pharmacol. 1998 Feb 19;343(2-3):201-7. [PubMed:9570468 ]
  4. Froimowitz M, Cody V: Biologically active conformers of phenothiazines and thioxanthenes. Further evidence for a ligand model of dopamine D2 receptor antagonists. J Med Chem. 1993 Jul 23;36(15):2219-27. [PubMed:8101879 ]
  5. Froimowitz M, Cody V: The incorporation of butyrophenones and related compounds into a pharmacophore for dopamine D2 antagonists. Drug Des Discov. 1997 Aug;15(2):63-81. [PubMed:9342550 ]
  6. Lang AE, Sandor P, Duff J: Remoxipride in Parkinson's disease: differential response in patients with dyskinesias fluctuations versus psychosis. Clin Neuropharmacol. 1995 Feb;18(1):39-45. [PubMed:8665533 ]
  7. 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. Li Z, Ichikawa J, Meltzer HY: A comparison of the effects of loxapine with ziprasidone and thioridazine on the release of dopamine and acetylcholine in the prefrontal cortex and nucleus accumbens. Psychopharmacology (Berl). 2003 May;167(3):315-23. Epub 2003 Mar 28. [PubMed:12664192 ]
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. Herrick-Davis K, Grinde E, Teitler M: Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors. J Pharmacol Exp Ther. 2000 Oct;295(1):226-32. [PubMed:10991983 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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.
Gene Name:
HTR5A
Uniprot ID:
P47898
Molecular Weight:
40254.69 Da
References
  1. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Receptor signaling protein activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling.
Gene Name:
ADRB1
Uniprot ID:
P08588
Molecular Weight:
51322.1 Da
References
  1. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Components:
NameUniProt IDDetails
D(1A) dopamine receptorP21728 Details
D(1B) dopamine receptorP21918 Details
References
  1. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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:
DRD5
Uniprot ID:
P21918
Molecular Weight:
52950.5 Da
References
  1. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Histamine receptor activity
Specific Function:
The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and differentiation. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase and, through a separate G protein-dependent mechanism, the phosphoinositide/protein kinase (PKC) si...
Gene Name:
HRH2
Uniprot ID:
P25021
Molecular Weight:
40097.65 Da
References
  1. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
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. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Serotonin:sodium symporter activity
Specific Function:
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into the pre-synaptic terminal for re-utilization. Plays a key role in mediating regulation of the availability of serotonin to other receptors of serotonergic systems. Terminates the action of serotonin an...
Gene Name:
SLC6A4
Uniprot ID:
P31645
Molecular Weight:
70324.165 Da
References
  1. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Norepinephrine:sodium symporter activity
Specific Function:
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A2
Uniprot ID:
P23975
Molecular Weight:
69331.42 Da
References
  1. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Monoamine transmembrane transporter activity
Specific Function:
Amine transporter. Terminates the action of dopamine by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A3
Uniprot ID:
Q01959
Molecular Weight:
68494.255 Da
References
  1. PDSP Ki Database [Link]
Comments
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Drug created on June 13, 2005 07:24 / Updated on July 26, 2016 01:53