Identification

Name
Loxapine
Accession Number
DB00408  (APRD00574)
Type
Small Molecule
Groups
Approved
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 IDs
AZ-004 / BRN 0626753 / CL 62,362 / CL 62362 / CL 71563 / CL-62362 / HF 3170 / LW 3170 / S 805 / SUM 3170 / SUM-3170 / UNII-376MYL4MAL / UNII-LER583670J / UNII-X59SG0MRYU
Product Ingredients
IngredientUNIICASInChI Key
Loxapine hydrochloride376MYL4MAL54810-23-0JSXBVMKACNEMKY-UHFFFAOYSA-N
Loxapine succinateX59SG0MRYU27833-64-3YQZBAXDVDZTKEQ-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AdasuvePowder, metered9.1 mgRespiratory (inhalation)Ferrer Internacional S.A.2013-02-20Not applicableEu
AdasuvePowder, metered4.5 mgRespiratory (inhalation)Ferrer Internacional S.A.2013-02-20Not applicableEu
AdasuveAerosol, powder10 mg/1Respiratory (inhalation)Galen Us Incorporated2017-09-26Not applicableUs
AdasuvePowder, metered4.5 mgRespiratory (inhalation)Ferrer Internacional S.A.2013-02-20Not applicableEu
AdasuveAerosol, powder10 mg/1Respiratory (inhalation)Teva Select Brands2014-01-22Not applicableUs
AdasuvePowder, metered9.1 mgRespiratory (inhalation)Ferrer Internacional S.A.2013-02-20Not applicableEu
AdasuveAerosol, powder10 mg/1Respiratory (inhalation)Alexza Pharmaceuticals, Inc.2012-12-212013-06-14Us
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
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-loxapineTablet50 mgOralApotex Corporation1998-03-30Not applicableCanada
Apo-loxapineTablet10 mgOralApotex Corporation1998-03-30Not applicableCanada
Apo-loxapineTablet5 mgOralApotex Corporation1998-03-30Not applicableCanada
Apo-loxapineTablet25 mgOralApotex Corporation1998-03-30Not applicableCanada
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
LoxapineCapsule10 mg/1OralAmerincan Health Packaging2013-04-152018-01-31Us
LoxapineTablet10 mg/1OralMarlex Pharmaceuticals Inc2014-10-01Not applicableUs
International/Other Brands
Cloxazepine / Lopac (Newai Chem) / Losagen (Patron) / Loxapac (Wyeth) / Rosup (Swiss Pharm)
Categories
UNII
LER583670J
CAS number
1977-10-2
Weight
Average: 327.808
Monoisotopic: 327.11383992
Chemical Formula
C18H18ClN3O
InChI Key
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

Pharmacology

Indication

For the management of the manifestations of psychotic disorders such as schizophrenia

Associated Conditions
Pharmacodynamics

Loxapine, 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 action

Loxapine 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.

TargetActionsOrganism
AD(2) dopamine receptor
antagonist
Human
UD(1A) dopamine receptor
antagonist
Human
A5-hydroxytryptamine receptor 2A
antagonist
Human
U5-hydroxytryptamine receptor 2C
antagonist
Human
U5-hydroxytryptamine receptor 1A
binder
Human
U5-hydroxytryptamine receptor 1B
binder
Human
U5-hydroxytryptamine receptor 1D
binder
Human
U5-hydroxytryptamine receptor 1E
binder
Human
U5-hydroxytryptamine receptor 3A
binder
Human
U5-hydroxytryptamine receptor 5A
binder
Human
U5-hydroxytryptamine receptor 6
binder
Human
U5-hydroxytryptamine receptor 7
binder
Human
UAlpha-1A adrenergic receptor
binder
Human
UAlpha-1B adrenergic receptor
binder
Human
UAlpha-2A adrenergic receptor
binder
Human
UAlpha-2B adrenergic receptor
binder
Human
UAlpha-2C adrenergic receptor
binder
Human
UBeta-1 adrenergic receptor
binder
Human
UMuscarinic acetylcholine receptor M1
binder
Human
UMuscarinic acetylcholine receptor M2
binder
Human
UMuscarinic acetylcholine receptor M3
binder
Human
UMuscarinic acetylcholine receptor M4
binder
Human
UMuscarinic acetylcholine receptor M5
binder
Human
UD(1) dopamine receptor
binder
Human
UD(3) dopamine receptor
binder
Human
UD(4) dopamine receptor
binder
Human
UD(1B) dopamine receptor
binder
Human
UHistamine H1 receptor
binder
Human
UHistamine H2 receptor
binder
Human
UHistamine H4 receptor
binder
Human
USodium-dependent serotonin transporter
binder
Human
USodium-dependent noradrenaline transporter
binder
Human
USodium-dependent dopamine transporter
binder
Human
Absorption

Systemic bioavailability of the parent drug was only about one third that after an equivalent intramuscular dose (25 mg base) in male volunteers

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

Hepatic

Route of elimination

Metabolites are excreted in the urine in the form of conjugates and in the feces unconjugated.

Half life

Oral-4 hours

Clearance
Not Available
Toxicity

LD50=65 mg/kg (Orally in mice)

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of serotonin syndrome can be increased when Loxapine is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of serotonin syndrome can be increased when 2,5-Dimethoxy-4-ethylthioamphetamine is combined with Loxapine.
3,4-MethylenedioxyamphetamineThe risk or severity of serotonin syndrome can be increased when 3,4-Methylenedioxyamphetamine is combined with Loxapine.
3,5-DinitrocatecholThe therapeutic efficacy of 3,5-Dinitrocatechol can be decreased when used in combination with Loxapine.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of serotonin syndrome can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Loxapine.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when Loxapine is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of serotonin syndrome can be increased when 5-methoxy-N,N-dimethyltryptamine is combined with Loxapine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when Loxapine is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe risk or severity of serotonin syndrome can be increased when Loxapine is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Loxapine.
Food Interactions
  • Take with food to reduce irritation. Avoid alcohol.

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
Human Metabolome Database
HMDB0014552
KEGG Drug
D02340
KEGG Compound
C07104
PubChem Compound
3964
PubChem Substance
46505047
ChemSpider
3827
BindingDB
22871
ChEBI
50841
ChEMBL
CHEMBL831
Therapeutic Targets Database
DAP000311
PharmGKB
PA450273
IUPHAR
205
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Loxapine
ATC Codes
N05AH01 — Loxapine
AHFS Codes
  • 28:16.08.92 — Miscellaneous Antipsychotics

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableBipolar1
1CompletedNot AvailableHealthy Volunteers1
1CompletedTreatmentAsthma Bronchial1
1CompletedTreatmentMigraines1
2CompletedTreatmentSchizophrenic Disorders1
2RecruitingTreatmentPain, Neuropathic1
3CompletedTreatmentBipolar I Disorder1
3CompletedTreatmentSchizophrenic Patients With Acute Agitation1
3TerminatedTreatmentAcute Agitated Patients1
4CompletedOtherHealthy Volunteers1
4CompletedTreatmentRestlessness1
4TerminatedTreatmentHaloperidol Causing Adverse Effects in Therapeutic Use / Lorazepam Causing Adverse Effects in Therapeutic Use / Loxapine Causing Adverse Effects in Therapeutic Use / Psychomotor Agitation1
Not AvailableCompletedNot AvailableBipolar Disorder (BD) / Psychotic Disorder NOS / Schizoaffective Disorders / Schizophrenic Disorders / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailablePsychomotor Agitation1
Not AvailableCompletedNot AvailableSchizophrenic Disorders1
Not AvailableCompletedTreatmentPsychomotor Agitation / Respiratory Insufficiency1
Not AvailableRecruitingNot AvailablePsychomotor Agitation1

Pharmacoeconomics

Manufacturers
  • Watson laboratories inc
  • Actavis totowa llc
  • Mylan pharmaceuticals inc
Packagers
  • Actavis Group
  • Amerisource Health Services Corp.
  • Major Pharmaceuticals
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Pharmaceutical Utilization Management Program VA Inc.
  • Physicians Total Care Inc.
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • UDL Laboratories
  • Watson Pharmaceuticals
Dosage forms
FormRouteStrength
Aerosol, powderRespiratory (inhalation)10 mg/1
Powder, meteredRespiratory (inhalation)4.5 mg
Powder, meteredRespiratory (inhalation)9.1 mg
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)
US7078020No2001-10-262021-10-26Us
US7052679No2001-10-262021-10-26Us
US7537009No2004-10-282024-10-28Us
US8173107No2001-10-262021-10-26Us
US8074644No2002-07-252022-07-25Us
US8991387No2004-05-212024-05-21Us
US8955512No2001-10-262021-10-26Us
US7601337No2001-10-262021-10-26Us
US8235037No2001-10-262021-10-26Us
US7585493No2001-10-262021-10-26Us
US7458374No2004-08-182024-08-18Us
US6716416No2002-05-202022-05-20Us
US8387612No2006-10-232026-10-23Us
US7090830No2001-10-262021-10-26Us
US9370629No2004-05-202024-05-20Us
US9440034No2001-10-262021-10-26Us
US9439907No2001-10-262021-10-26Us
US9687487No2001-10-262021-10-26Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)109-111 °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 RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-0a4l-7590000000-118f30ca0699bf2b3d2e
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00ai-0149000000-d463f8ddf4248264d132
MS/MS Spectrum - , positiveLC-MS/MSsplash10-01r6-0930000000-4798aec046d747300d80

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzoxazepines
Sub Class
Dibenzoxazepines
Direct Parent
Dibenzoxazepines
Alternative Parents
Diarylethers / N-methylpiperazines / Imidolactams / Benzenoids / Aryl chlorides / Trialkylamines / Propargyl-type 1,3-dipolar organic compounds / Oxacyclic compounds / Carboxamidines / Azacyclic compounds
show 3 more
Substituents
Dibenzoxazepine / Diaryl ether / N-methylpiperazine / N-alkylpiperazine / Aryl chloride / Aryl halide / 1,4-diazinane / Piperazine / Benzenoid / Imidolactam
show 19 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
dibenzoxazepine (CHEBI:50841)

Targets

Details
1. D(2) dopamine receptor
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
Uniprot Name
D(2) dopamine receptor
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
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
Uniprot Name
D(1A) dopamine receptor
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
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-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
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-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
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...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
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 subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
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 subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
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 trig...
Gene Name
HTR1E
Uniprot ID
P28566
Uniprot Name
5-hydroxytryptamine receptor 1E
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-gate...
Gene Name
HTR3A
Uniprot ID
P46098
Uniprot Name
5-hydroxytryptamine receptor 3A
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 ...
Gene Name
HTR5A
Uniprot ID
P47898
Uniprot Name
5-hydroxytryptamine receptor 5A
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 ...
Gene Name
HTR6
Uniprot ID
P50406
Uniprot Name
5-hydroxytryptamine receptor 6
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 ...
Gene Name
HTR7
Uniprot ID
P34969
Uniprot Name
5-hydroxytryptamine receptor 7
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) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
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) prot...
Gene Name
ADRA1B
Uniprot ID
P35368
Uniprot Name
Alpha-1B adrenergic receptor
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 oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
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...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
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
Uniprot Name
Alpha-2C adrenergic receptor
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 e...
Gene Name
ADRB1
Uniprot ID
P08588
Uniprot Name
Beta-1 adrenergic receptor
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...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
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...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
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...
Gene Name
CHRM3
Uniprot ID
P20309
Uniprot Name
Muscarinic acetylcholine receptor M3
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...
Gene Name
CHRM4
Uniprot ID
P08173
Uniprot Name
Muscarinic acetylcholine receptor M4
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...
Gene Name
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
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:
References
  1. PDSP Ki Database [Link]
Details
25. D(3) dopamine receptor
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
Uniprot Name
D(3) dopamine receptor
Molecular Weight
44224.335 Da
References
  1. PDSP Ki Database [Link]
Details
26. D(4) dopamine receptor
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 ...
Gene Name
DRD4
Uniprot ID
P21917
Uniprot Name
D(4) dopamine receptor
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
Uniprot Name
D(1B) dopamine receptor
Molecular Weight
52950.5 Da
References
  1. PDSP Ki Database [Link]
Details
28. Histamine H1 receptor
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 catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
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 diff...
Gene Name
HRH2
Uniprot ID
P25021
Uniprot Name
Histamine H2 receptor
Molecular Weight
40097.65 Da
References
  1. PDSP Ki Database [Link]
Details
30. Histamine H4 receptor
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 agoni...
Gene Name
HRH4
Uniprot ID
Q9H3N8
Uniprot Name
Histamine H4 receptor
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 t...
Gene Name
SLC6A4
Uniprot ID
P31645
Uniprot Name
Sodium-dependent serotonin transporter
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
Uniprot Name
Sodium-dependent noradrenaline transporter
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
Uniprot Name
Sodium-dependent dopamine transporter
Molecular Weight
68494.255 Da
References
  1. PDSP Ki Database [Link]

Drug created on June 13, 2005 07:24 / Updated on September 22, 2018 22:22