General
Preferred name
(S)-dimetindene
Synonyms
(S)-(+)-Dimethindene maleate ()
dimethindene-(S)-(+) ()
(S)-(+)-Dimethindene (maleate) ()
P&D ID
PD070792
CAS
136152-65-3
Tags
available
drug
Drug indication
Pruritus
Drug Status
approved
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION (S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48)[1].
PRICE 230
DESCRIPTION (S)-(+)-Dimethindene maleate is an orally available, selective muscarinic M2 receptor and histamine H1 receptor antagonist that also inhibits muscarinic M1, M3, and M4 receptors.
DESCRIPTION This is the (S)-enantiomer of the antihistamine drug . (GtoPdb)
DESCRIPTION M2-selective antagonist (Tocriscreen Total)
DESCRIPTION Highly selective, orally active non-peptide ETA antagonist (Tocris Bioactive Compound Library)
DESCRIPTION The maleate salt form of (S)-(+)-Dimethindene, which has been found to be a subtype-selective mAChR M2 antagonist and histamine H1 receptor antagonist. (BOC Sciences Bioactive Compounds)
Compound Sets
10
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
DrugMAP Approved Drugs
Guide to Pharmacology
JUMP-MOA Compound Set
MedChem Express Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Total
External IDs
24
Properties
(calculated by RDKit )
Molecular Weight
292.19
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
0
Rotatable Bonds
5
Ring Count
3
Aromatic Ring Count
2
cLogP
4.15
TPSA
16.13
Fraction CSP3
0.35
Chiral centers
1.0
Largest ring
6.0
QED
0.82
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Primary Target
M2 Receptors
MOA
Antagonist
cholinergic receptor antagonist, histamine receptor antagonist
acetylcholine receptor antagonist
Indication
allergic rhinitis
Target
HRH1
Histamine Receptor
mAChR
Therapeutic Class
Antiinflammatory Agents
Pathway
GPCR/G protein
Immunology/Inflammation
Neuronal Signaling
Source data