General
Preferred name
clemastine
Synonyms
CLEMASTINE FUMARATE ()
Meclastine (fumarate) ()
HS-592 (fumarate) ()
Meclastine fumarate ()
Clemastine (fumarate) ()
Meclastine (fumarate)HS-592 (fumarate)Meclastine fumarate ()
Clemastine hydrochloride ()
Hydroxyclemastine ()
Clemastine (HS-592) fumarate ()
HS-592 fumarate, Meclastine fumarate ()
Clemastine hydrogen fumarate ()
Tavegil ()
Tavist-1 ()
Tavist ()
HS-592 ()
NSC-756685 ()
Clemastin ()
P&D ID
PD010126
CAS
14976-57-9
15686-51-8
Tags
nuisance
natural product
drug
available
Approved by
FDA
First approval
1977
Drug Status
investigational
approved
Drug indication
Discovery agent
Allergic rhinitis
Antihistaminic
Max Phase
Phase 4
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PHARMACODYNAMICS Clemastine is an antihistamine that also induces anticholinergic and sedative effects. Antihistamines competitively antagonize various physiological effects of histamine including increased capillary permeability and dilatation, the formation of edema, the "flare" and "itch" response, and gastrointestinal and respiratory smooth muscle constriction. Within the vascular tree, H1- receptor antagonists inhibit both the vasoconstrictor and vasodilator effects of histamine. Depending on the dose, H1- receptor antagonists can produce CNS stimulation or depression. Most antihistamines exhibit central and/or peripheral anticholinergic activity. Antihistamines act by competitively blocking H1- receptor sites. Antihistamines do not pharmacologically antagonize or chemically inactivate histamine, nor do they prevent the release of histamine.
DESCRIPTION Marketed formulations contain clemastine hydrogen fumarate (PubChem CID 5281069). (GtoPdb)
DESCRIPTION H1 antagonist (Tocriscreen Plus)
DESCRIPTION H1 antagonist (Tocriscreen Total)
DESCRIPTION Potent and selective 5-HT1B and 5-HT1D antagonist (Tocris Bioactive Compound Library)
DESCRIPTION Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. (BOC Sciences Bioactive Compounds)
DESCRIPTION Clemastine is a histamine H1 antagonist commonly used for the symptoms of allergic rhinitis, hay fever, and cold. (BOC Sciences Bioactive Compounds)
Cell lines
0
Organisms
5
Compound Sets
32
AdooQ Bioactive Compound Library
A10226
BOC Sciences Bioactive Compounds
clemastine-fumarate-cas-14976-57-9-item-84-59335
clemastine-cas-15686-51-8-item-59873
Cayman Chemical Bioactives
14637
ChEMBL Approved Drugs
CHEMBL1200795
CHEMBL1626
ChEMBL Drugs
CHEMBL1200795
CHEMBL1626
Concise Guide to Pharmacology 2017/18
6063
Concise Guide to Pharmacology 2019/20
6063
Concise Guide to Pharmacology 2021/22
6063
Concise Guide to Pharmacology 2023/24
6063
Drug Repurposing Hub
DrugBank
DB00283
DrugBank Approved Drugs
DB00283
DrugCentral
671
DrugCentral Approved Drugs
671
DrugMAP
DM5DOEC
DMBZWQL
DrugMAP Approved Drugs
DMBZWQL
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
EOS101014
Guide to Pharmacology
6063
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1626
MedChem Express Bioactive Compound Library
HY-B0298A
NCATS Inxight Approved Drugs
95QN29S1ID
NPC Screening Collection
Nuisance compounds in cellular assays
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
Clemastine-Fumarate
TargetMol Bioactive Compound Library
T0147
The Spectrum Collection
Tocris Bioactive Compound Library
1453
Tocriscreen Plus
1453
Tocriscreen Total
External IDs
58
Properties
(calculated by RDKit )
Molecular Weight
343.17
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
0
Rotatable Bonds
6
Ring Count
3
Aromatic Ring Count
2
cLogP
5.1
TPSA
12.47
Fraction CSP3
0.43
Chiral centers
2.0
Largest ring
6.0
QED
0.72
Structural alerts
1
CAD
Nuisance compounds in cellular assays
Related compounds
Custom attributes
(extracted from source data)
Target Type
7-TM Receptors
Pathway
GPCR/G protein
Immunology/Inflammation
Neuroscience
Neuronal Signaling
Target
H1 receptor
HRH1
Histamine Receptor
Autophagy,Histamine Receptor,mTOR
Primary Target
Histamine H1 Receptors
MOA
Antagonist
Histamine Receptor antagonist
Indication
allergic rhinitis, urticaria
Therapeutic Class
Antiallergic Agents
Source data