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Identification
NameCyproheptadine
Accession NumberDB00434  (APRD00033)
TypeSmall Molecule
GroupsApproved
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 Identifiers
  • Fl 5967
  • HSp 1229
Approved Prescription ProductsNot Available
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cyproheptadinesyrup2 mg/5mLoralPharmaceutical Associates, Inc.2013-07-29Not applicableUs
Cyproheptadinesyrup2 mg/5mLoralPharmaceutical Associates, Inc.2013-07-29Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralREMEDYREPACK INC.2011-09-20Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralTeva Pharmaceuticals USA Inc2009-01-23Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralPhysicians Total Care, Inc.2003-05-21Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralState of Florida DOH Central Pharmacy2014-11-01Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralREMEDYREPACK INC.2011-09-22Not applicableUs
Cyproheptadine Hydrochloridesyrup2 mg/5mLoralCarilion Materials Management2006-07-10Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralAv Kare, Inc.2010-06-15Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralCarilion Materials Management2010-06-15Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralMirror Pharmaceuticals LLC2015-09-23Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2010-01-08Not applicableUs
Cyproheptadine Hydrochloridesyrup2 mg/5mLoralRising Pharmaceuticals, Inc.2006-07-10Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralREMEDYREPACK INC.2013-12-312016-04-05Us
Cyproheptadine Hydrochloridesyrup2 mg/5mLoralActavis Mid Atlantic LLC2009-07-31Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralCore Pharma, Llc2015-07-29Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralREMEDYREPACK INC.2012-08-16Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralC.O. Truxton, Inc.2010-06-15Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralbryant ranch prepack2009-01-23Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralBreckenridge Pharmaceutical, Inc.2013-10-21Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralCardinal Health2010-06-15Not applicableUs
Cyproheptadine Hydrochloridetablet4 mg/1oralIngenus Pharmaceuticals Llc2015-09-23Not applicableUs
Cyproheptadine Hydrochloridesyrup2 mg/5mLoralPhysicians Total Care, Inc.2009-07-31Not applicableUs
Approved Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cyproheptadine 4mg Tabletstablet4 mgoralJamp Pharma Corporation2010-05-03Not applicableCanada
Euro-cyproheptadine 2mg/5mlsyrup2 mgoralEuro Pharm International Canada Inc2003-05-27Not applicableCanada
Euro-cyproheptadine 4mg/tablettablet4 mgoralEuro Pharm International Canada Inc2006-06-05Not 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
Unapproved/Other Products Not Available
International Brands
NameCompany
ApeplusRadicura
ApitupUniversal
BioheptBiofarm
CiplactinCipla
CipractineTeriak
CiproheptadinaArena
CiprovitNot Available
CiptadineIBN
CyheptineGreater Pharma
CyllerminCCPC
PeriactinMerck
PeriactineTeofarma
PeriatinApex
ReactinOrion
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Cyproheptadine Hydrochloride
Thumb
  • InChI Key: ZPMVNZLARAEGHB-UHFFFAOYSA-N
  • Monoisotopic Mass: 323.144077416
  • Average Mass: 323.859
DBSALT000625
Categories
UNII2YHB6175DO
CAS number129-03-3
WeightAverage: 287.3981
Monoisotopic: 287.167399677
Chemical FormulaC21H21N
InChI KeyInChIKey=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
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as dibenzocycloheptenes. These are compounds containing a dibenzocycloheptene moiety, which consists of two benzene connected by a cycloheptene ring.
KingdomOrganic compounds
Super ClassBenzenoids
ClassDibenzocycloheptenes
Sub ClassNot Available
Direct ParentDibenzocycloheptenes
Alternative Parents
Substituents
  • Dibenzocycloheptene
  • Piperidine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor 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.
PharmacodynamicsCyproheptadine 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 actionCyproheptadine 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.
Related Articles
AbsorptionWell absorbed after oral administration.
Volume of distributionNot Available
Protein binding96 to 99%
Metabolism

Hepatic (cytochrome P-450 system) and some renal.

Route of eliminationAfter 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 lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
Pharmacoeconomics
Manufacturers
  • Merck and co inc
Packagers
Dosage forms
FormRouteStrength
Syruporal2 mg/5mL
Tabletoral4 mg/1
Syruporal2 mg
Syruporal0.4 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.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point112.3-113-3Engelhardt, 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 RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (10 KB)
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-00kr-2290000000-a17c27a9f171b058f2c3View in MoNA
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
ATC CodesR06AX02
AHFS Codes
  • 04:04.92
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (74.3 KB)
Interactions
Drug Interactions
Drug
AclidiniumAclidinium may increase the anticholinergic activities of Cyproheptadine.
AmphetamineAmphetamine may decrease the sedative activities of Cyproheptadine.
AzelastineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Cyproheptadine.
Benzylpenicilloyl PolylysineCyproheptadine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Cyproheptadine.
Botulinum Toxin Type ACyproheptadine may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BCyproheptadine may increase the anticholinergic activities of Botulinum Toxin Type B.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
BuprenorphineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CathinoneCathinone may decrease the sedative activities of Cyproheptadine.
Cimetropium BromideCyproheptadine may increase the anticholinergic activities of Cimetropium Bromide.
CitalopramThe therapeutic efficacy of Citalopram can be decreased when used in combination with Cyproheptadine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
EluxadolineCyproheptadine may increase the activities of Eluxadoline.
EscitalopramThe therapeutic efficacy of Escitalopram can be decreased when used in combination with Cyproheptadine.
EthanolCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FluoxetineThe therapeutic efficacy of Fluoxetine can be decreased when used in combination with Cyproheptadine.
FluvoxamineThe therapeutic efficacy of Fluvoxamine can be decreased when used in combination with Cyproheptadine.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Glucagon recombinant.
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Cyproheptadine.
HydrocodoneCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Cyproheptadine.
IsocarboxazidIsocarboxazid may increase the anticholinergic activities of Cyproheptadine.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Cyproheptadine.
LinezolidLinezolid may increase the anticholinergic activities of Cyproheptadine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Cyproheptadine.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
MethotrimeprazineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetyrosineCyproheptadine may increase the sedative activities of Metyrosine.
MianserinMianserin may increase the anticholinergic activities of Cyproheptadine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
MirabegronThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Mirabegron.
MirtazapineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MoclobemideMoclobemide may increase the anticholinergic activities of Cyproheptadine.
MorphineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Morphine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
OrphenadrineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe therapeutic efficacy of Paroxetine can be decreased when used in combination with Cyproheptadine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
PhenelzinePhenelzine may increase the anticholinergic activities of Cyproheptadine.
Potassium ChlorideCyproheptadine may increase the ulcerogenic activities of Potassium Chloride.
PramipexoleCyproheptadine may increase the sedative activities of Pramipexole.
PramlintidePramlintide may increase the anticholinergic activities of Cyproheptadine.
ProcarbazineProcarbazine may increase the anticholinergic activities of Cyproheptadine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Cyproheptadine.
RamosetronCyproheptadine may increase the activities of Ramosetron.
RasagilineRasagiline may increase the anticholinergic activities of Cyproheptadine.
RopiniroleCyproheptadine may increase the sedative activities of Ropinirole.
RotigotineCyproheptadine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Cyproheptadine.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Cyproheptadine.
SelegilineSelegiline may increase the anticholinergic activities of Cyproheptadine.
SertralineThe therapeutic efficacy of Sertraline can be decreased when used in combination with Cyproheptadine.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Cyproheptadine.
SuvorexantCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineThe therapeutic efficacy of Cyproheptadine can be decreased when used in combination with Tacrine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
Tedizolid PhosphateTedizolid Phosphate may increase the anticholinergic activities of Cyproheptadine.
ThalidomideCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TiotropiumCyproheptadine may increase the anticholinergic activities of Tiotropium.
TopiramateThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Topiramate.
TranylcypromineTranylcypromine may increase the anticholinergic activities of Cyproheptadine.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Cyproheptadine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Cyproheptadine.
VilazodoneThe therapeutic efficacy of Vilazodone can be decreased when used in combination with Cyproheptadine.
VortioxetineThe therapeutic efficacy of Vortioxetine can be decreased when used in combination with Cyproheptadine.
ZolpidemCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Avoid alcohol.
  • Take with food.

Targets

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 catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
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-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
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-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modul...
Gene Name:
HTR2C
Uniprot ID:
P28335
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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM1
Uniprot ID:
P11229
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 action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
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 action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM3
Uniprot ID:
P20309
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 ]

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 regulator of isoform 1.
Gene Name:
UGT1A3
Uniprot ID:
P35503
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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on April 10, 2014 11:16