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

Similar Structures

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

Contraindications & Blackbox Warnings

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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	antagonist	Humans
A5-hydroxytryptamine receptor 2A	antagonist	Humans
A5-hydroxytryptamine receptor 2C	antagonist	Humans
UMuscarinic acetylcholine receptor M1	antagonist	Humans
UMuscarinic acetylcholine receptor M2	antagonist	Humans
UMuscarinic acetylcholine receptor M3	antagonist	Humans
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

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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 Data
Acebutolol	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 Description

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Extended description of the mechanism of action and particular properties of each drug interaction.

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Severity

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A severity rating for each drug interaction, from minor to major.

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Evidence Level

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Action

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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

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
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Cyproheptadine Hydrochloride	Tablet	4 mg/1	Oral	Boscogen, Inc.	2010-06-15	Not applicable

Additional Data Available

Application Number

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A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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Product Code

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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
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Cyproheptadine	Syrup	2 mg/5mL	Oral	Solubiomix	2018-05-03	2018-06-27
Cyproheptadine	Syrup	2 mg/5mL	Oral	Pharmaceutical Associates, Inc.	2013-07-29	Not applicable
Cyproheptadine	Syrup	2 mg/5mL	Oral	Pharmaceutical Associates, Inc.	2013-07-29	Not applicable
Cyproheptadine Hydrochloride	Tablet	4 mg/1	Oral	Marlex Pharmaceuticals Inc	2018-01-01	Not applicable
Cyproheptadine Hydrochloride	Tablet	4 mg/1	Oral	Par Pharmaceutical	1981-07-09	2013-09-30
Cyproheptadine Hydrochloride	Tablet	4 mg/1	Oral	bryant ranch prepack	2017-07-20	Not applicable
Cyproheptadine Hydrochloride	Tablet	4 mg/1	Oral	bryant ranch prepack	2018-04-11	Not applicable
Cyproheptadine Hydrochloride	Tablet	4 mg/1	Oral	State of Florida DOH Central Pharmacy	2009-07-01	Not applicable
Cyproheptadine Hydrochloride	Tablet	4 mg/1	Oral	Appco Pharma Llc	2016-12-14	2017-01-16
Cyproheptadine Hydrochloride	Syrup	2 mg/5mL	Oral	Physicians Total Care, Inc.	2009-07-31	Not applicable

Additional Data Available

Application Number

Available for Purchase

A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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Product Code

Available 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	Route	Labeller	Marketing Start	Marketing End
Unlock Additional Data
Cyproheptadine 4mg Tablets	Tablet	Oral	Jamp Pharma Corporation	2010-05-03	Not applicable
Euro-cyproheptadine 2mg/5ml	Syrup	Oral	Euro Pharm International Canada Inc	Not applicable	Not applicable
Euro-cyproheptadine 4 Mg/tablet	Tablet	Oral	Euro Pharm International Canada Inc	Not applicable	Not applicable
Jamp Cyproheptadine Syrup	Syrup	Oral	Jamp Pharma Corporation	Not applicable	Not applicable
Periactin Syr 2mg/5ml	Syrup	Oral	Merck Frosst Canada & Cie, Merck Frosst Canada & Co.	1961-12-31	2002-07-29
Periactin Tab 4mg	Tablet	Oral	Merck Frosst Canada & Cie, Merck Frosst Canada & Co.	1961-12-31	2002-07-29
PMS-cyproheptadine HCl Tab 4mg	Tablet	Oral	Pharmascience Inc	1996-10-16	Not applicable
Sandoz Cyproheptadine	Syrup	Oral	Sandoz Canada Incorporated	2003-05-27	Not applicable
Sandoz Cyproheptadine Tablet	Tablet	Oral	Sandoz Canada Incorporated	2006-06-05	2019-11-25

Additional Data Available

Application Number

Available for Purchase

A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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Product Code

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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
RxNav: 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

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Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Attention Deficit and Disruptive Behavior Disorders / Attention Deficit Disorder With Hyperactivity / Attention Deficit Hyperactivity Disorder (ADHD) / Attention Deficit/Hyperactivity Disorder / Mental Disorders Diagnosed in Childhood	1
4	Terminated	Treatment	Feeding Behaviors	1
4	Unknown Status	Treatment	Failure to Thrive	1
3	Terminated	Supportive Care	Malignancies	1
2	Completed	Supportive Care	Cachexia / Leukemias / Malignant Lymphomas / Myelodysplastic Syndromes (MDS) / Myelodysplastic/Myeloproliferative Diseases / Neoplasms, Brain / Tumors of the Central Nervous System / Unspecified Childhood Solid Tumor, Protocol Specific	1
2	Completed	Treatment	Alcohol Dependence	1
2	Recruiting	Treatment	Alcohol Use Disorder (AUD)	1
2	Terminated	Supportive Care	Leukemias / Malignant Lymphomas / Malnutrition / Myelodysplastic Syndromes (MDS) / Unspecified Childhood Solid Tumor, Protocol Specific / Weight Changes	1
2	Terminated	Treatment	Functional Abdominal Pain	1
0	Completed	Basic Science	Stroke	1

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
Tablet	Oral	4 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	4 MG
Syrup		50 mg/5mL
Syrup	Oral	0.4 MG/ML
Syrup	Oral	40 mg
Syrup	Oral
Tablet	Oral
Syrup	Oral	240 ml
Tablet	Oral	4.5 MG
Tablet, film coated	Oral	4 MG
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

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

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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

Property	Measurement	pH	Temperature (°C)	References
Kd (nM)	5400	N/A	N/A	16220969
Ki (nM)	0.06	N/A	N/A	7925364

Details1. Histamine H1 receptor

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]

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	0.46	N/A	N/A	9225287 / 22694093
Ki (nM)	1.6	N/A	N/A	11266163
Ki (nM)	2.88	N/A	N/A	7984267
Ki (nM)	3	N/A	N/A	15081025

Details2. 5-hydroxytryptamine receptor 2A

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]

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	11	N/A	N/A	15081025
Ki (nM)	2.23	N/A	N/A	9225287

Details3. 5-hydroxytryptamine receptor 2C

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]

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	12	N/A	N/A	8100134

Details4. Muscarinic acetylcholine receptor M1

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]

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	7	N/A	N/A	8100134

Details5. Muscarinic acetylcholine receptor M2

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]

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	12	N/A	N/A	8100134

Details6. Muscarinic acetylcholine receptor M3

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]

Details7. 5-hydroxytryptamine receptor 7

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

Details1. UDP-glucuronosyltransferase 1-3

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 January 25, 2021 22:38

Cyproheptadine

Identification

Structure for Cyproheptadine (DB00434)

Pharmacology

Learn about our commercial Contraindications & Blackbox Warnings data.

Learn about our commercial Adverse Effects data.

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Targets

References

References

References

References

References

References

References

Enzymes

References