General
Preferred name
(S)-(+)-Dimethindene maleate
Synonyms
(S)-(+)-Dimethindene (maleate) ()
P&D ID
PD021904
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 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)
DESCRIPTION M2-selective antagonist (Tocriscreen Total)
DESCRIPTION Highly selective, orally active non-peptide ETA antagonist (Tocris Bioactive Compound Library)
Compound Sets
7
BOC Sciences Bioactive Compounds
s-dimethindene-maleate-cas-136152-65-3-item-169779
CZ-OPENSCREEN Bioactive Library
DrugMAP
DMMHNU2
DrugMAP Approved Drugs
DMMHNU2
MedChem Express Bioactive Compound Library
HY-107647
Tocris Bioactive Compound Library
1425
Tocriscreen Total
External IDs
9
Properties
(calculated by RDKit )
Molecular Weight
408.2
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
2
Rotatable Bonds
7
Ring Count
3
Aromatic Ring Count
2
cLogP
3.86
TPSA
90.73
Fraction CSP3
0.29
Chiral centers
1.0
Largest ring
6.0
QED
0.68
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Primary Target
M2 Receptors
MOA
Antagonist
Therapeutic Class
Antiinflammatory Agents
Pathway
GPCR/G protein
Immunology/Inflammation
Neuronal Signaling
Target
Histamine Receptor
mAChR
Source data