Identification
- Summary
Loxapine is a antipsychotic used for the treatment of schizophrenia.
- Brand Names
- Adasuve, Xylac
- Generic Name
- Loxapine
- DrugBank Accession Number
- DB00408
- Background
An antipsychotic agent used in schizophrenia. [PubChem]
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Loxapine (DB00408)
- Weight
- Average: 327.808
Monoisotopic: 327.11383992 - Chemical Formula
- C18H18ClN3O
- Synonyms
- 2-Chloro-11-(4-methyl-1-piperazinyl)dibenz[b,f][1,4]oxazepine
- 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
Pharmacology
- Indication
For the management of the manifestations of psychotic disorders such as schizophrenia
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Acute agitation •••••••••••• •••••••• Treatment of Acute agitation •••••••••••• •••••••• Management of Schizophrenia •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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.
- 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
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
LD50=65 mg/kg (Orally in mice)
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Loxapine is combined with 1,2-Benzodiazepine. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Loxapine. Acenocoumarol The risk or severity of adverse effects can be increased when Loxapine is combined with Acenocoumarol. Acetazolamide The risk or severity of CNS depression can be increased when Loxapine is combined with Acetazolamide. Acetophenazine The risk or severity of CNS depression can be increased when Loxapine is combined with Acetophenazine. - Food Interactions
- Avoid alcohol.
- Take with food. Food reduces irritation.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Loxapine hydrochloride 376MYL4MAL 54810-23-0 JSXBVMKACNEMKY-UHFFFAOYSA-N Loxapine succinate X59SG0MRYU 27833-64-3 YQZBAXDVDZTKEQ-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Cloxazepine / Lopac (Newai Chem) / Losagen (Patron) / Loxapac (Wyeth) / Rosup (Swiss Pharm)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Adasuve Powder, metered 4.5 mg Respiratory (inhalation) Ferrer Internacional S.A. 2016-09-07 Not applicable EU 
Adasuve Aerosol, powder 10 mg/1 Respiratory (inhalation) Alexza Pharmaceuticals, Inc. 2022-05-31 Not applicable US 
Adasuve Aerosol, powder 10 mg/1 Respiratory (inhalation) Teva Select Brands 2014-01-22 2018-01-31 US Adasuve Powder, metered 9.1 mg Respiratory (inhalation) Ferrer Internacional S.A. 2016-09-07 Not applicable EU Adasuve Powder, metered 9.1 mg Respiratory (inhalation) Ferrer Internacional S.A. 2016-09-07 Not applicable EU - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-loxapine Tablet 25 mg Oral Apotex Corporation 1998-03-30 Not applicable Canada 
Apo-loxapine Tablet 5 mg Oral Apotex Corporation 1998-03-30 Not applicable Canada Apo-loxapine Tablet 50 mg Oral Apotex Corporation 1998-03-30 Not applicable Canada Apo-loxapine Tablet 10 mg Oral Apotex Corporation 1998-03-30 Not applicable Canada Dom-loxapine Tablets 10mg Tablet 10 mg Oral Dominion Pharmacal 1999-09-15 Not applicable Canada
Categories
- ATC Codes
- N05AH01 — Loxapine
- Drug Categories
- Antidepressive Agents
- Antipsychotic Agents
- Antipsychotic Agents (First Generation [Typical])
- Central Nervous System Agents
- Central Nervous System Depressants
- Diazepines, Oxazepines, Thiazepines and Oxepines
- Dibenzoxazepines
- Dopamine Agents
- Dopamine Antagonists
- Dopamine D2 Receptor Antagonists
- Drugs causing inadvertant photosensitivity
- Heterocyclic Compounds, Fused-Ring
- Miscellaneous Antipsychotics
- Nervous System
- Neurotoxic agents
- Neurotransmitter Agents
- P-glycoprotein inhibitors
- Photosensitizing Agents
- Psycholeptics
- Psychotropic Drugs
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin 5-HT2 Receptor Antagonists
- Serotonin 5-HT2A Receptor Antagonists
- Serotonin 5-HT2C Receptor Antagonists
- Serotonin Agents
- Serotonin Receptor Antagonists
- Tranquilizing Agents
- Chemical TaxonomyProvided by Classyfire
- 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
- 1,4-diazinane / Amidine / Amine / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Carboxylic acid amidine / Diaryl ether show 19 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- dibenzoxazepine (CHEBI:50841)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- LER583670J
- CAS number
- 1977-10-2
- 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[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,9,12,14-heptaene
- SMILES
- CN1CCN(CC1)C1=NC2=CC=CC=C2OC2=C1C=C(Cl)C=C2
References
- Synthesis Reference
U.S. Patents 3,412,193; 3,546,226.
US3412193- General References
- Glazer WM: Does loxapine have "atypical" properties? Clinical evidence. J Clin Psychiatry. 1999;60 Suppl 10:42-6. [Article]
- 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. [Article]
- External Links
- Human Metabolome Database
- HMDB0014552
- KEGG Drug
- D02340
- KEGG Compound
- C07104
- PubChem Compound
- 3964
- PubChem Substance
- 46505047
- ChemSpider
- 3827
- BindingDB
- 22871
- 6475
- ChEBI
- 50841
- ChEMBL
- CHEMBL831
- ZINC
- ZINC000019796158
- Therapeutic Targets Database
- DAP000311
- PharmGKB
- PA450273
- Guide to Pharmacology
- GtP Drug Page
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Loxapine
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Other Healthy Subjects (HS) 2 4 Completed Treatment Restlessness 1 4 Terminated Treatment Haloperidol Causing Adverse Effects in Therapeutic Use / Lorazepam Causing Adverse Effects in Therapeutic Use / Loxapine Causing Adverse Effects in Therapeutic Use / Psychomotor Agitation 1 3 Completed Treatment Bipolar 1 Disorder 1 3 Completed Treatment Patients With Schizophrenia and Acute Agitation 1
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
Form Route Strength Aerosol, powder Respiratory (inhalation) 10 mg/1 Powder Respiratory (inhalation) 10 mg Powder, metered Respiratory (inhalation) 4.5 MG Powder, metered Respiratory (inhalation) 9.1 MG Aerosol, powder Respiratory (inhalation) 9.1 mg Capsule Oral Tablet Oral 50 mg / tab Solution Intramuscular 50 mg / mL Liquid Intramuscular 50 mg / mL Liquid Oral 25 mg / mL Tablet Oral 13.6 mg / tab Tablet Oral 34 mg / tab Tablet Oral 68 mg / tab Tablet Oral 6.8 mg / tab Capsule Oral 10 mg/1 Capsule Oral 25 mg/1 Capsule Oral 5 mg/1 Capsule Oral 50 mg/1 Tablet Oral 10 mg/1 Tablet Oral 25 mg/1 Tablet Oral 5 mg/1 Tablet Oral 50 mg/1 Tablet Oral 10 mg / tab Tablet Oral 25 mg / tab Tablet Oral 5 mg / tab Solution Oral 25 mg / mL Tablet Oral 10 mg Tablet Oral 2.5 mg Tablet Oral 25 mg Tablet Oral 5 mg Tablet Oral 50 mg - Prices
Unit description Cost Unit Loxapac 50 mg/ml 7.05USD ml Loxitane 50 mg capsule 4.04USD capsule Loxitane 25 mg capsule 3.09USD capsule Loxapine 50 mg capsule 2.57USD capsule Loxitane 10 mg capsule 2.04USD capsule Loxapine 25 mg capsule 1.92USD capsule Loxitane 5 mg capsule 1.58USD capsule Loxapine 10 mg capsule 1.27USD capsule Loxapine Succinate 5 mg capsule 1.03USD capsule Loxapine 5 mg capsule 0.99USD capsule Pms-Loxapine 50 mg Tablet 0.54USD tablet Pms-Loxapine 25 mg Tablet 0.41USD tablet Pms-Loxapine 10 mg Tablet 0.26USD tablet Pms-Loxapine 5 mg Tablet 0.16USD tablet Pms-Loxapine 2.5 mg Tablet 0.08USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US7078020 No 2006-07-18 2021-10-26 US US7052679 No 2006-05-30 2021-10-26 US US7537009 No 2009-05-26 2024-10-28 US US8173107 No 2012-05-08 2021-10-26 US US8074644 No 2011-12-13 2022-07-25 US US8991387 No 2015-03-31 2024-05-21 US US8955512 No 2015-02-17 2021-10-26 US US7601337 No 2009-10-13 2021-10-26 US US8235037 No 2012-08-07 2021-10-26 US US7585493 No 2009-09-08 2021-10-26 US US7458374 No 2008-12-02 2024-08-18 US US6716416 No 2004-04-06 2022-05-20 US US8387612 No 2013-03-05 2026-10-23 US US7090830 No 2006-08-15 2021-10-26 US US9370629 No 2016-06-21 2024-05-20 US US9440034 No 2016-09-13 2021-10-26 US US9439907 No 2016-09-13 2021-10-26 US US9687487 No 2017-06-27 2021-10-26 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 109-111 °C U.S. Patents 3,412,193; 3,546,226. logP 3.6 Not Available - Predicted Properties
Property Value Source Water Solubility 0.103 mg/mL ALOGPS logP 3.18 ALOGPS logP 3.46 Chemaxon logS -3.5 ALOGPS pKa (Strongest Basic) 7.18 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 28.07 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 95.11 m3·mol-1 Chemaxon Polarizability 34.99 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9944 Blood Brain Barrier + 0.9801 Caco-2 permeable + 0.5531 P-glycoprotein substrate Substrate 0.8545 P-glycoprotein inhibitor I Inhibitor 0.8525 P-glycoprotein inhibitor II Inhibitor 0.8388 Renal organic cation transporter Inhibitor 0.7084 CYP450 2C9 substrate Non-substrate 0.7331 CYP450 2D6 substrate Substrate 0.7155 CYP450 3A4 substrate Substrate 0.6309 CYP450 1A2 substrate Inhibitor 0.8159 CYP450 2C9 inhibitor Non-inhibitor 0.8755 CYP450 2D6 inhibitor Inhibitor 0.7543 CYP450 2C19 inhibitor Non-inhibitor 0.6217 CYP450 3A4 inhibitor Non-inhibitor 0.9393 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6968 Ames test Non AMES toxic 0.9133 Carcinogenicity Non-carcinogens 0.8743 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 3.3057 LD50, mol/kg Not applicable hERG inhibition (predictor I) Strong inhibitor 0.5701 hERG inhibition (predictor II) Inhibitor 0.6141
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 180.6828823 predictedDarkChem Lite v0.1.0 [M-H]- 169.25868 predictedDeepCCS 1.0 (2019) [M+H]+ 181.0752823 predictedDarkChem Lite v0.1.0 [M+H]+ 171.61668 predictedDeepCCS 1.0 (2019) [M+Na]+ 180.4241823 predictedDarkChem Lite v0.1.0 [M+Na]+ 177.70982 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein group
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- PDSP Ki Database [Link]
- Kind
- Protein
- Organism
- Humans
- 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
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55