Identification

Name
Cyproheptadine
Accession Number
DB00434  (APRD00033)
Type
Small Molecule
Groups
Approved
Description

A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc. [PubChem]

Structure
Thumb
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
  • Axoprol
  • Ciproheptadina
  • Cyproheptadin
  • Cyproheptadine
  • Cyproheptadinum
  • Dihexazin
  • Glutodina
External IDs
Fl 5967 / HSp 1229
Product Ingredients
IngredientUNIICASInChI Key
Cyproheptadine Hydrochloride0S9323MCT0969-33-5ZPMVNZLARAEGHB-UHFFFAOYSA-N
Product Images
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CyproheptadineSyrup2 mg/5mLOralPharmaceutical Associates, Inc.2013-07-29Not applicableUs
CyproheptadineSyrup2 mg/5mLOralSolubiomix2018-05-032018-06-27Us
CyproheptadineSyrup2 mg/5mLOralPharmaceutical Associates, Inc.2013-07-29Not applicableUs
Cyproheptadine HydrochlorideTablet4 mg/1OralRemedy Repack2012-08-162013-08-17Us
Cyproheptadine HydrochlorideTablet4 mg/1OralIngenus Pharmaceuticals Llc2015-09-23Not applicableUs
Cyproheptadine HydrochlorideTablet4 mg/1Oralbryant ranch prepack2017-07-20Not applicableUs
Cyproheptadine HydrochlorideTablet4 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs2010-01-08Not applicableUs
Cyproheptadine HydrochlorideTablet4 mg/1OralCypress Pharmaceuticals, Inc.2010-06-152013-09-11Us
Cyproheptadine HydrochlorideTablet4 mg/1OralRemedy Repack2017-06-05Not applicableUs
Cyproheptadine HydrochlorideSyrup2 mg/5mLOralActavis Pharma Company2009-07-272018-12-31Us
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cyproheptadine 4mg TabletsTablet4 mgOralJamp Pharma Corporation2010-05-03Not applicableCanada
Euro-cyproheptadine 2mg/5mlSyrup2 mgOralSandoz Canada Incorporated2003-05-27Not applicableCanada
Euro-cyproheptadine 2mg/5mlSyrup2 mgOralEuro Pharm International Canada IncNot applicableNot applicableCanada
Euro-cyproheptadine 4 Mg/tabletTablet4 mgOralEuro Pharm International Canada IncNot applicableNot applicableCanada
Euro-cyproheptadine 4mg/tabletTablet4 mgOralSandoz Canada Incorporated2006-06-05Not applicableCanada
Jamp Cyproheptadine SyrupSyrup0.4 mgOralJamp Pharma CorporationNot applicableNot applicableCanada
Periactin Syr 2mg/5mlSyrup2 mgOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1961-12-312002-07-29Canada
Periactin Tab 4mgTablet4 mgOralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1961-12-312002-07-29Canada
PMS-cyproheptadine HCl Tab 4mgTablet4 mgOralPharmascience Inc1996-10-16Not applicableCanada
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)
Categories
UNII
2YHB6175DO
CAS number
129-03-3
Weight
Average: 287.3981
Monoisotopic: 287.167399677
Chemical Formula
C21H21N
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

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
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.

TargetActionsOrganism
AHistamine H1 receptor
antagonist
Human
A5-hydroxytryptamine receptor 2A
antagonist
Human
A5-hydroxytryptamine receptor 2C
antagonist
Human
UMuscarinic acetylcholine receptor M1
antagonist
Human
UMuscarinic acetylcholine receptor M2
antagonist
Human
UMuscarinic acetylcholine receptor M3
antagonist
Human
U5-hydroxytryptamine receptor 7Not AvailableHuman
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
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Cyproheptadine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(2-benzhydryloxyethyl)diethyl-methylammonium iodideThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with (2-benzhydryloxyethyl)diethyl-methylammonium iodide.
1,10-PhenanthrolineThe therapeutic efficacy of Cyproheptadine can be decreased when used in combination with 1,10-Phenanthroline.
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative and stimulatory activities of Cyproheptadine.
2,5-Dimethoxy-4-ethylthioamphetamine2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative and stimulatory activities of Cyproheptadine.
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative and stimulatory activities of Cyproheptadine.
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative and stimulatory activities of Cyproheptadine.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with 5-methoxy-N,N-dimethyltryptamine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
Food Interactions
  • Avoid alcohol.
  • Take with food.

References

Synthesis Reference

Engelhardt, E.L.; U S . Patent 3,014,911; December 26, 1961; assigned to Merck & Co., Inc.

General References
  1. 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
ChEBI
4046
ChEMBL
CHEMBL516
Therapeutic Targets Database
DAP000103
PharmGKB
PA164749366
IUPHAR
277
Guide to Pharmacology
GtP Drug Page
HET
C7H
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Cyproheptadine
ATC Codes
R06AX02 — Cyproheptadine
AHFS Codes
  • 04:04.92 — Miscellaneous Derivatives
PDB Entries
5ayf
MSDS
Download (74.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedBasic ScienceStrokes1
2CompletedSupportive CareCachexia / Leukemias / Malignant Lymphomas / Myelodysplastic Syndromes / Myelodysplastic/Myeloproliferative Diseases / Neoplasms, Brain / Tumors, Central Nervous System / Unspecified Childhood Solid Tumor, Protocol Specific1
2CompletedTreatmentAlcoholism1
2TerminatedSupportive CareLeukemias / Malignant Lymphomas / Malnutrition / Myelodysplastic Syndromes / Unspecified Childhood Solid Tumor, Protocol Specific / Weight Changes1
2Unknown StatusTreatmentFunctional Abdominal Pain1
3TerminatedSupportive CareCancers1
4CompletedTreatmentAttention Deficit and Disruptive Behavior Disorders / Attention Deficit Disorder With Hyperactivity / Attention Deficit Disorder With Hyperactivity (ADHD) / Mental Disorders Diagnosed in Childhood1
4Not Yet RecruitingTreatmentFeeding Behaviors1
4Unknown StatusTreatmentFailure to Thrive1
Not AvailableCompletedBasic ScienceSpinal Cord Injuries (SCI)1
Not AvailableRecruitingDiagnosticNausea1
Not AvailableRecruitingTreatmentHemiparesis / Muscle Spasticity / Strokes1

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
FormRouteStrength
SyrupOral2 mg/5mL
SolutionOral2 mg/5mL
TabletOral4 mg/1
SyrupOral0.4 mg
SyrupOral2 mg
TabletOral4 mg
Prices
Unit descriptionCostUnit
Cyproheptadine hcl powder7.34USD g
Cyproheptadine HCl 4 mg tablet0.47USD tablet
Cyproheptadine 4 mg tablet0.43USD tablet
Cyproheptadine HCl 2 mg/5ml Syrup0.16USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)112.3-113-3Engelhardt, E.L.; U S . Patent 3,014,911; December 26, 1961; assigned to Merck & Co., Inc.
water solubilitySolubleNot Available
logP4.69SANGSTER (1993)
Predicted Properties
PropertyValueSource
Water Solubility0.0136 mg/mLALOGPS
logP5.02ALOGPS
logP4.38ChemAxon
logS-4.3ALOGPS
pKa (Strongest Basic)8.05ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area3.24 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity105.17 m3·mol-1ChemAxon
Polarizability34.17 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.986
Caco-2 permeable+0.8038
P-glycoprotein substrateSubstrate0.8598
P-glycoprotein inhibitor IInhibitor0.8563
P-glycoprotein inhibitor IINon-inhibitor0.5315
Renal organic cation transporterInhibitor0.8303
CYP450 2C9 substrateNon-substrate0.8127
CYP450 2D6 substrateNon-substrate0.6719
CYP450 3A4 substrateSubstrate0.6092
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9082
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.902
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5433
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.9511
BiodegradationNot ready biodegradable0.8349
Rat acute toxicity2.9576 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5429
hERG inhibition (predictor II)Inhibitor0.7423
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (10 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-00kr-2290000000-a17c27a9f171b058f2c3
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
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-0290000000-964629904e89d79568d8

Taxonomy

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
Dibenzocycloheptene / Piperidine / Tertiary aliphatic amine / Tertiary amine / Azacycle / Organoheterocyclic compound / Organic nitrogen compound / Organopnictogen compound / Hydrocarbon derivative / Organonitrogen compound
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
piperidines, tertiary amine (CHEBI:4046)

Targets

Details
1. Histamine H1 receptor
Kind
Protein
Organism
Human
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
  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. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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
Human
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
  1. 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
Human
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
  1. 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
Human
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
  1. 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
Human
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
  1. 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
Human
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
  1. 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
Human
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
  1. 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 September 23, 2018 19:37