Cyproheptadine
Identification
- Name
- Cyproheptadine
- Accession Number
- DB00434
- Description
A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Cyproheptadine (DB00434)
- Weight
- Average: 287.3981
Monoisotopic: 287.167399677 - Chemical Formula
- C21H21N
- Synonyms
- 1-methyl-4-(5-dibenzo(a,e)cycloheptatrienylidene)piperidine
- 1-Methyl-4-(5H-dibenzo(a,d)cycloheptenylidene)piperidine
- 4-(5-dibenzo(a,d)cyclohepten-5-ylidine)-1-methylpiperidine
- 4-(5H-dibenzo(a,d)cyclohepten-5-ylidene)-1-methylpiperidine
- 4-Dibenzo[a,d]cyclohepten-5-ylidene-1-methyl-piperidine
- 5-(1-methylpiperidylidene-4)-5H-dibenzo(a,d)cyclopheptene
- Ciproheptadina
- Cyproheptadin
- Cyproheptadine
- Cyproheptadinum
- External IDs
- Fl 5967
- HSp 1229
Pharmacology
- Indication
For treatment of perennial and seasonal allergic rhinitis, vasomotor rhinitis, allergic conjunctivitis due to inhalant allergens and foods, mild uncomplicated allergic skin manifestations of urticaria and angioedema, amelioration of allergic reactions to blood or plasma, cold urticaria, dermatographism, and as therapy for anaphylactic reactions adjunctive to epinephrine.
- Associated Conditions
- Allergic Reactions
- Anaphylaxis
- Anorexia Nervosa (AN)
- Cold urticaria
- Conjunctivitis, Seasonal Allergic
- Cushing's Disease
- Decreased appetite caused by Chronic disease
- Dermatographic urticaria
- Migraine
- Seasonal Allergic Rhinitis (SAR)
- Sexual dysfunction caused by antipsychotic agents
- Sexual dysfunction caused by fluoxetine
- Sexual dysfunction caused by monoamine oxidase inhibitors
- Sexual dysfunction caused by tricyclic antidepressants
- Vasomotor Rhinitis
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- Pharmacodynamics
Cyproheptadine is a piperidine antihistamine. Unlike other antihistamines, this drug also antagonizes serotonin receptors. This action makes Cyproheptadine useful in conditions such as vascular headache and anorexia. Cyproheptadine does not prevent the release of histamine but rather competes with free histamine for binding at HA-receptor sites. Cyproheptadine competitively antagonizes the effects of histamine on HA-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. Most antihistamines possess significant anticholinergic properties, but Cyproheptadine exerts only weak anticholinergic actions. Blockade of central muscarinic receptors appears to account for Cyproheptadine's antiemetic effects, although the exact mechanism is unknown. Cyproheptadine also competes with serotonin at receptor sites in smooth muscle in the intestines and other locations. Antagonism of serotonin on the appetite center of the hypothalamus may account for Cyproheptadine's ability to stimulate appetite. Cyproheptadine also has been used to counter vascular headaches, which many believe are caused by changes in serotonin activity, however it is unclear how Cyproheptadine exerts a beneficial effect on this condition.
- Mechanism of action
Cyproheptadine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Cyproheptadine also competes with serotonin at receptor sites in smooth muscle in the intestines and other locations. Antagonism of serotonin on the appetite center of the hypothalamus may account for Cyproheptadine's ability to stimulate appetite.
Target Actions Organism AHistamine H1 receptor antagonistHumans A5-hydroxytryptamine receptor 2A antagonistHumans A5-hydroxytryptamine receptor 2C antagonistHumans UMuscarinic acetylcholine receptor M1 antagonistHumans UMuscarinic acetylcholine receptor M2 antagonistHumans UMuscarinic acetylcholine receptor M3 antagonistHumans U5-hydroxytryptamine receptor 7 Not Available Humans - Absorption
Well absorbed after oral administration.
- Volume of distribution
- Not Available
- Protein binding
96 to 99%
- Metabolism
Hepatic (cytochrome P-450 system) and some renal.
- Route of elimination
After a single 4 mg oral dose of14C-labelled cyproheptadine HCl in normal subjects, given as tablets 2% to 20% of the radioactivity was excreted in the stools. At least 40% of the administered radioactivity was excreted in the urine.
- Half-life
- Not Available
- Clearance
- Not Available
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- Toxicity
- Not Available
- Affected organisms
- Humans and other mammals
- Pathways
Pathway Category Cyproheptadine H1-Antihistamine Action Drug action - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- 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 Unlock Additional DataAcebutolol The risk or severity of QTc prolongation can be increased when Cyproheptadine is combined with Acebutolol. Acenocoumarol The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Acenocoumarol. Acetazolamide Acetazolamide may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine. Acetophenazine Acetophenazine may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine. Aclidinium The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Aclidinium. Acrivastine The risk or severity of QTc prolongation can be increased when Cyproheptadine is combined with Acrivastine. Adenosine The risk or severity of QTc prolongation can be increased when Cyproheptadine is combined with Adenosine. Agomelatine The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Agomelatine. Ajmaline The risk or severity of QTc prolongation can be increased when Cyproheptadine is combined with Ajmaline. Alfentanil The risk or severity of adverse effects can be increased when Alfentanil is combined with Cyproheptadine. Additional Data Available- Extended DescriptionExtended DescriptionAvailable for Purchase
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - SeveritySeverityAvailable for Purchase
A severity rating for each drug interaction, from minor to major.
Learn more - Evidence LevelEvidence LevelAvailable for Purchase
A rating for the strength of the evidence supporting each drug interaction.
Learn more - ActionActionAvailable for Purchase
An effect category for each drug interaction. Know how this interaction affects the subject drug.
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- Food Interactions
- Avoid alcohol.
- Take with food.
Products
Purchasing individual compounds or compound libraries for your research?
Learn More- Product Ingredients
Ingredient UNII CAS InChI Key Cyproheptadine hydrochloride 0S9323MCT0 969-33-5 ZPMVNZLARAEGHB-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Apeplus (Radicura) / Apitup (Universal) / Biohept (Biofarm) / Ciplactin (Cipla) / Cipractine (Teriak) / Ciproheptadina (Arena) / Ciprovit / Ciptadine (IBN) / Cyheptine (Greater Pharma) / Cyllermin (CCPC) / Periactin (Merck) / Periactine (Teofarma) / Periatin (Apex) / Reactin (Orion)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataCyproheptadine Hydrochloride Tablet 4 mg/1 Oral Boscogen, Inc. 2010-06-15 Not applicable US 
Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable for Purchase
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataCyproheptadine Syrup 2 mg/5mL Oral Pharmaceutical Associates, Inc. 2013-07-29 Not applicable US Cyproheptadine Syrup 2 mg/5mL Oral Solubiomix 2018-05-03 2018-06-27 US Cyproheptadine Syrup 2 mg/5mL Oral Pharmaceutical Associates, Inc. 2013-07-29 Not applicable US Cyproheptadine Hydrochloride Tablet 4 mg/1 Oral State of Florida DOH Central Pharmacy 2009-07-01 Not applicable US Cyproheptadine Hydrochloride Tablet 4 mg/1 Oral REMEDYREPACK INC. 2017-06-05 Not applicable US Cyproheptadine Hydrochloride Tablet 4 mg/1 Oral Cadila Healthcare Limited 2017-07-20 Not applicable US Cyproheptadine Hydrochloride Syrup 2 mg/5mL Oral Rising Pharmaceuticals, Inc. 2006-07-10 Not applicable US Cyproheptadine Hydrochloride Tablet 4 mg/1 Oral Apnar Pharma 2018-05-15 Not applicable US Cyproheptadine Hydrochloride Tablet 4 mg/1 Oral Remedy Repack 2010-08-12 2012-05-02 US Cyproheptadine Hydrochloride Tablet 4 mg/1 Oral Proficient Rx LP 2017-02-21 Not applicable US Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable for Purchase
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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- Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataCyproheptadine 4mg Tablets Tablet Oral Jamp Pharma Corporation 2010-05-03 Not applicable Canada 
Euro-cyproheptadine 2mg/5ml Syrup Oral Euro Pharm International Canada Inc Not applicable Not applicable Canada Euro-cyproheptadine 4 Mg/tablet Tablet Oral Euro Pharm International Canada Inc Not applicable Not applicable Canada Jamp Cyproheptadine Syrup Syrup Oral Jamp Pharma Corporation Not applicable Not applicable Canada Periactin Syr 2mg/5ml Syrup Oral Merck Frosst Canada & Cie, Merck Frosst Canada & Co. 1961-12-31 2002-07-29 Canada Periactin Tab 4mg Tablet Oral Merck Frosst Canada & Cie, Merck Frosst Canada & Co. 1961-12-31 2002-07-29 Canada PMS-cyproheptadine HCl Tab 4mg Tablet Oral Pharmascience Inc 1996-10-16 Not applicable Canada Sandoz Cyproheptadine Syrup Oral Sandoz Canada Incorporated 2003-05-27 Not applicable Canada Sandoz Cyproheptadine Tablet Tablet Oral Sandoz Canada Incorporated 2006-06-05 2019-11-25 Canada Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable for Purchase
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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Categories
- ATC Codes
- R06AX02 — Cyproheptadine
- Drug Categories
- Agents producing tachycardia
- Agents that reduce seizure threshold
- Anti-Allergic Agents
- Anticholinergic Agents
- Antidepressive Agents
- Antihistamines for Systemic Use
- Antipruritics
- Benzocycloheptenes
- Central Nervous System Depressants
- Dermatologicals
- Dibenzocycloheptenes
- Drugs causing inadvertant photosensitivity
- Gastrointestinal Agents
- Histamine Agents
- Histamine Antagonists
- Histamine H1 Antagonists
- Miscellaneous Derivatives
- Muscarinic Antagonists
- Neurotransmitter Agents
- Photosensitizing Agents
- Piperidines
- Potential QTc-Prolonging Agents
- QTc Prolonging Agents
- Serotonin 5-HT2 Receptor Antagonists
- Serotonin 5-HT2A Receptor Antagonists
- Serotonin 5-HT2C Receptor Antagonists
- Serotonin Agents
- Serotonin Receptor Antagonists
- UGT1A3 substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as dibenzocycloheptenes. These are compounds containing a dibenzocycloheptene moiety, which consists of two benzene rings connected by a cycloheptene ring.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Dibenzocycloheptenes
- Sub Class
- Not Available
- Direct Parent
- Dibenzocycloheptenes
- Alternative Parents
- Piperidines / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
- Substituents
- Amine / Aromatic heteropolycyclic compound / Azacycle / Dibenzocycloheptene / Hydrocarbon derivative / Organic nitrogen compound / Organoheterocyclic compound / Organonitrogen compound / Organopnictogen compound / Piperidine
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- piperidines, tertiary amine (CHEBI:4046)
Chemical Identifiers
- UNII
- 2YHB6175DO
- CAS number
- 129-03-3
- InChI Key
- JJCFRYNCJDLXIK-UHFFFAOYSA-N
- InChI
- InChI=1S/C21H21N/c1-22-14-12-18(13-15-22)21-19-8-4-2-6-16(19)10-11-17-7-3-5-9-20(17)21/h2-11H,12-15H2,1H3
- IUPAC Name
- 1-methyl-4-{tricyclo[9.4.0.0³,⁸]pentadeca-1(15),3,5,7,9,11,13-heptaen-2-ylidene}piperidine
- SMILES
- CN1CCC(CC1)=C1C2=CC=CC=C2C=CC2=CC=CC=C12
References
- Synthesis Reference
Engelhardt, E.L.; U S . Patent 3,014,911; December 26, 1961; assigned to Merck & Co., Inc.
- General References
- Tokunaga S, Takeda Y, Shinomiya K, Hirase M, Kamei C: Effects of some H1-antagonists on the sleep-wake cycle in sleep-disturbed rats. J Pharmacol Sci. 2007 Feb;103(2):201-6. Epub 2007 Feb 8. [PubMed:17287588]
- External Links
- Human Metabolome Database
- HMDB0014578
- KEGG Compound
- C06935
- PubChem Compound
- 2913
- PubChem Substance
- 46508613
- ChemSpider
- 2810
- BindingDB
- 50017721
- 3013
- ChEBI
- 4046
- ChEMBL
- CHEMBL516
- ZINC
- ZINC000000968264
- Therapeutic Targets Database
- DAP000103
- PharmGKB
- PA164749366
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- C7H
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Cyproheptadine
- AHFS Codes
- 04:04.92 — Miscellaneous Derivatives
- PDB Entries
- 5ayf
- MSDS
- Download (74.3 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Merck and co inc
- Packagers
- Actavis Group
- Amerisource Health Services Corp.
- Apotheca Inc.
- Atlantic Biologicals Corporation
- Bryant Ranch Prepack
- Cardinal Health
- Chestertown Home Medical Supplies
- Corepharma LLC
- Cypress Pharmaceutical Inc.
- Dept Health Central Pharmacy
- Direct Dispensing Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Emcure Pharmaceuticals Ltd.
- Heartland Repack Services LLC
- Ivax Pharmaceuticals
- Lake Erie Medical and Surgical Supply
- Lyne Laboratories Inc.
- Major Pharmaceuticals
- Medisca Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Palmetto Pharmaceuticals Inc.
- Par Pharmaceuticals
- PCA LLC
- PD-Rx Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Pliva Inc.
- Prepak Systems Inc.
- Qualitest
- Remedy Repack
- Resource Optimization and Innovation LLC
- Rising Pharmaceuticals
- Southwood Pharmaceuticals
- Stason Pharmaceuticals Inc.
- Teva Pharmaceutical Industries Ltd.
- Tya Pharmaceuticals
- Vangard Labs Inc.
- Dosage Forms
Form Route Strength Capsule 2 mg Tablet Oral 2 mg Capsule 4 mg Syrup Oral 0.04 g Syrup 2 mg/5mL Syrup Oral 2 mg/5mL Powder Not applicable 1 g/1g Solution Oral 2 mg/5mL Syrup Oral 1.5 mg/5mL Tablet Oral 4 mg/1 Tablet, coated Oral 4 mg Tablet, sugar coated Oral Syrup 50 mg/5mL Syrup Oral 0.4 MG/ML Tablet Oral 4 mg Syrup Oral 40 mg Syrup Oral Tablet Oral Syrup Oral 240 ml Tablet Oral 4.5 MG Tablet, film coated Oral Solution / drops Oral 2 mg/5mL Tablet, coated Oral 2 mg Powder, for solution Oral 0.035 g Elixir Oral 2 mg/5mL - Prices
Unit description Cost Unit Cyproheptadine hcl powder 7.34USD g Cyproheptadine HCl 4 mg tablet 0.47USD tablet Cyproheptadine 4 mg tablet 0.43USD tablet Cyproheptadine HCl 2 mg/5ml Syrup 0.16USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 112.3-113-3 Engelhardt, E.L.; U S . Patent 3,014,911; December 26, 1961; assigned to Merck & Co., Inc. water solubility Soluble Not Available logP 4.69 SANGSTER (1993) - Predicted Properties
Property Value Source Water Solubility 0.0136 mg/mL ALOGPS logP 5.02 ALOGPS logP 4.38 ChemAxon logS -4.3 ALOGPS pKa (Strongest Basic) 8.05 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 1 ChemAxon Hydrogen Donor Count 0 ChemAxon Polar Surface Area 3.24 Å2 ChemAxon Rotatable Bond Count 0 ChemAxon Refractivity 105.17 m3·mol-1 ChemAxon Polarizability 34.17 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 + 1.0 Blood Brain Barrier + 0.986 Caco-2 permeable + 0.8038 P-glycoprotein substrate Substrate 0.8598 P-glycoprotein inhibitor I Inhibitor 0.8563 P-glycoprotein inhibitor II Non-inhibitor 0.5315 Renal organic cation transporter Inhibitor 0.8303 CYP450 2C9 substrate Non-substrate 0.8127 CYP450 2D6 substrate Non-substrate 0.6719 CYP450 3A4 substrate Substrate 0.6092 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.9082 CYP450 2D6 inhibitor Inhibitor 0.8932 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.902 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.5433 Ames test Non AMES toxic 0.9132 Carcinogenicity Non-carcinogens 0.9511 Biodegradation Not ready biodegradable 0.8349 Rat acute toxicity 2.9576 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.5429 hERG inhibition (predictor II) Inhibitor 0.7423
Spectra
- Mass Spec (NIST)
- Download (10 KB)
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Mass Spectrum (Electron Ionization) MS splash10-00kr-2290000000-a17c27a9f171b058f2c3 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available MS/MS Spectrum - , positive LC-MS/MS splash10-000i-0290000000-964629904e89d79568d8
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Histamine receptor activity
- Specific Function
- In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
- Gene Name
- HRH1
- Uniprot ID
- P35367
- Uniprot Name
- Histamine H1 receptor
- Molecular Weight
- 55783.61 Da
References
- 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
- 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
- Rashid M, Nakazawa M, Nagatomo T: Effects of sarpogrelate, a novel 5-HT2 antagonist, on 5-HT-induced endothelium-dependent relaxations in porcine coronary artery. Jpn J Pharmacol. 2002 Aug;89(4):405-12. [PubMed:12233819]
- Honda M, Nishida T, Ono H: Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors. Eur J Pharmacol. 2003 Jan 1;458(1-2):91-9. [PubMed:12498911]
- Callaway CW, Rempel N, Peng RY, Geyer MA: Serotonin 5-HT1-like receptors mediate hyperactivity in rats induced by 3,4-methylenedioxymethamphetamine. Neuropsychopharmacology. 1992 Sep;7(2):113-27. [PubMed:1358088]
- Hoenicke EM, Vanecek SA, Woods JH: The discriminative stimulus effects of clozapine in pigeons: involvement of 5-hydroxytryptamine1C and 5-hydroxytryptamine2 receptors. J Pharmacol Exp Ther. 1992 Oct;263(1):276-84. [PubMed:1403790]
- Calka O, Metin A, Dulger H, Erkoc R: Effect of cyproheptadine on serum leptin levels. Adv Ther. 2005 Sep-Oct;22(5):424-8. [PubMed:16418149]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- 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
- Honda M, Nishida T, Ono H: Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors. Eur J Pharmacol. 2003 Jan 1;458(1-2):91-9. [PubMed:12498911]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Phosphatidylinositol phospholipase c activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM1
- Uniprot ID
- P11229
- Uniprot Name
- Muscarinic acetylcholine receptor M1
- Molecular Weight
- 51420.375 Da
References
- Eltze M, Lambrecht G, Mutschler E: Cyproheptadine displays high affinity for muscarinic receptors but does not discriminate between receptor subtypes. Eur J Pharmacol. 1989 Dec 7;173(2-3):219-22. [PubMed:2625138]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- G-protein coupled acetylcholine receptor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM2
- Uniprot ID
- P08172
- Uniprot Name
- Muscarinic acetylcholine receptor M2
- Molecular Weight
- 51714.605 Da
References
- Eltze M, Lambrecht G, Mutschler E: Cyproheptadine displays high affinity for muscarinic receptors but does not discriminate between receptor subtypes. Eur J Pharmacol. 1989 Dec 7;173(2-3):219-22. [PubMed:2625138]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Receptor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM3
- Uniprot ID
- P20309
- Uniprot Name
- Muscarinic acetylcholine receptor M3
- Molecular Weight
- 66127.445 Da
References
- Eltze M, Lambrecht G, Mutschler E: Cyproheptadine displays high affinity for muscarinic receptors but does not discriminate between receptor subtypes. Eur J Pharmacol. 1989 Dec 7;173(2-3):219-22. [PubMed:2625138]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
- Teitler M, Toohey N, Knight JA, Klein MT, Smith C: Clozapine and other competitive antagonists reactivate risperidone-inactivated h5-HT7 receptors: radioligand binding and functional evidence for GPCR homodimer protomer interactions. Psychopharmacology (Berl). 2010 Dec;212(4):687-97. doi: 10.1007/s00213-010-2001-x. Epub 2010 Sep 9. [PubMed:20827463]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Retinoic acid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
- Gene Name
- UGT1A3
- Uniprot ID
- P35503
- Uniprot Name
- UDP-glucuronosyltransferase 1-3
- Molecular Weight
- 60337.835 Da
References
- Green MD, King CD, Mojarrabi B, Mackenzie PI, Tephly TR: Glucuronidation of amines and other xenobiotics catalyzed by expressed human UDP-glucuronosyltransferase 1A3. Drug Metab Dispos. 1998 Jun;26(6):507-12. [PubMed:9616184]
Drug created on June 13, 2005 07:24 / Updated on November 23, 2020 09:08
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