General
Preferred name
CYPROHEPTADINE
Synonyms
CYPROHEPTADINE HYDROCHLORIDE ()
Cyproheptadine hydrochloride sesquihydrate ()
Periactin hydrochloride ()
Peritol ()
Cyproheptadine HCl ()
Cyproheptadine (hydrochloride) ()
Cyproheptadine (hydrochloride sesquihydrate) ()
Periactin ()
Periactin hydrochloride, Peritol ()
Cyproheptadine hydrochloride hydrate ()
Cyproheptadine Hydrocloride ()
NSC-759282 ()
Periactine ()
NSC-169911 ()
Ciprovit ()
Cyproheptadine (hydrochloride hydrate) ()
Cyproheptadine-d3 ()
P&D ID
PD010029
CAS
969-33-5
41354-29-4
129-03-3
2712455-05-3
Tags
natural product
drug
available
Approved by
FDA
First approval
1961
Drug Status
approved
Drug indication
Antipruritic
Antihistaminic
Rhinitis
Max Phase
Phase 4
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Cyproheptadine is a histamine H1 receptor antagonist, and also antagonizes serotonin receptors.
(GtoPdb)
DESCRIPTION
5-HT2 serotonin receptor antagonist
(LOPAC library)
DESCRIPTION
5-HT2 antagonist
(Tocriscreen Total)
DESCRIPTION
Cyproheptadine is a non-selective histamine receptor antagonist for 5-HT2 receptor with IC50 of 0.6 nM. It is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties. It is also SETD7/9 inhibitor with IC50 value of 1μM. It decreases expression and increases degradation of estrogen receptor (ER) α in breast tumor MCF7 cells. It is used as antipruritic, antiallergic, appetite stimulant, and for the post-gastrectomy dumping syndrome and so on. It is also useful for migraine prophylactic.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
1
Compound Sets
36
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
DrugMatrix
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
Ki Database
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
NCATS Inxight Approved Drugs
NIH Clinical Collections (NCC)
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Other bioactive compounds
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
The Spectrum Collection
Tocriscreen Total
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
76
Molecular Weight
287.17
Hydrogen Bond Acceptors
1
Hydrogen Bond Donors
0
Rotatable Bonds
0
Ring Count
4
Aromatic Ring Count
2
cLogP
4.7
TPSA
3.24
Fraction CSP3
0.24
Chiral centers
0.0
Largest ring
7.0
QED
0.58
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Selectivity
5-HT2
Pathway
GPCR/G protein
Chromatin/Epigenetic
Neuroscience
Neuronal Signaling
Immunology/Inflammation
Apoptosis
Target
SETD7
SETD9
ADRA1A, ADRA1B, ADRA1D, CHRM1, CHRM2, CHRM3, HRH1, HTR2A, HTR2C, HTR6, HTR7
5-HT2A/H1 antagonist
5-HT Receptor
Histamine Receptor
5-HT Receptor,SETD
MOA
5-HT Receptor antagonist
Histone Methyltransferase inhibitor
Histamine H1 Receptor Antagonists
5-HT2B Antagonists
Histamine Receptor antagonist
Member status
member
Disease Area
allergy, otolaryngology, ophthalmology, dermatology
Indication
allergic rhinitis, vasomotor rhinitis, conjunctivitis, urticaria, dermatographism
Therapeutic Class
Antihistamines
Solubility
DMSO 65 mg/mL
Water <1 mg/mL
Source data
