General
Preferred name
MEPENZOLATE
Synonyms
MEPENZOLATE BROMIDE ()
Cantil ()
Cantilaque ()
Colibantil ()
AN-6437 ()
HY-17585 ()
NSC-4358 ()
Glycophenylate ()
Mepenzolone Bromide ()
FT-0671006 ()
Mepenzolate Methylbromide ()
mepenzolic acid ()
Mepenzolate cation ()
Mepenzolate ion ()
Mepenzolate bromide free base ()
Mepenzolate (Bromide) ()
P&D ID
PD009364
CAS
76-90-4
25990-43-6
Tags
available
drug
Approved by
FDA
First approval
1956
Drug Status
approved
Drug indication
Peptic ulcer
Gastrointestinal disease
Anticholinergic
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
In in vitro binding assays, (R)-mepenzolate has a higher affinity for the human M2 and M3 muscarinic acetylcholine receptors than (S)-mepenzolate .
(GtoPdb)
ABSORPTION
Between 3 and 22% of an orally administered dose is excreted in the urine over a 5-day period, with the majority of the radioactivity appearing on Day 1. The remainder appears in the next 5 days in the feces and presumably has not been absorbed.;
TOXICITY
The signs and symptoms of overdosage are headache; nausea; vomiting; blurred vision; dilated pupils; hot, dry skin; dizziness; dryness of the mouth; difficulty in swallowing; and CNS stimulation. A curare-like action may occur (i.e., neuromuscular blockade leading to muscular weakness and possible ; paralysis). The oral LD50 is greater than 750 mg/kg in mice and greater than 1000 mg/kg in rats. ; ;
INDICATION
For use as adjunctive therapy in the treatment of peptic ulcer. It has not been ; shown to be effective in contributing to the healing of peptic ulcer, decreasing the rate of recurrence, or preventing complications.;
PHARMACODYNAMICS
Mepenzolate diminishes gastric acid and pepsin secretion. Mepenzolate also suppresses spontaneous contractions of the colon. Pharmacologically, it is a post-ganglionic parasympathetic inhibitor.;
DESCRIPTION
Mepenzolate Bromide is a muscarinic antagonist used to treat gastrointestinal disorders, and decreases the severity of elastase-induced airspace enlargement and respiratory dysfunction.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
20
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
DrugMatrix
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
NIH Clinical Collections (NCC)
NPC Screening Collection
Pandemic Response Box
Prestwick Chemical Library
ReFrame library
TargetMol Bioactive Compound Library
The Spectrum Collection
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
39
Molecular Weight
340.19
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
3
Aromatic Ring Count
2
cLogP
2.7
TPSA
46.53
Fraction CSP3
0.38
Chiral centers
1.0
Largest ring
6.0
QED
0.69
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
Neuroscience
Target
mAChR
Therapeutic Class
Parasympatholytics
Source data
