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Details

Stereochemistry RACEMIC
Molecular Formula C21H26NO3
Molecular Weight 340.436
Optical Activity ( + / - )
Defined Stereocenters 0 / 2
E/Z Centers 0
Charge 1

SHOW SMILES / InChI
Structure of Mepenzolate

SMILES

C[N+]1(C)CCCC(C1)OC(=O)C(O)(C2=CC=CC=C2)C3=CC=CC=C3

InChI

InChIKey=GKNPSSNBBWDAGH-UHFFFAOYSA-N
InChI=1S/C21H26NO3/c1-22(2)15-9-14-19(16-22)25-20(23)21(24,17-10-5-3-6-11-17)18-12-7-4-8-13-18/h3-8,10-13,19,24H,9,14-16H2,1-2H3/q+1

HIDE SMILES / InChI

Description

Mepenzolate is a postganglionic parasympathetic inhibitor. It decreases gastric acid and pepsin secretion and suppresses spontaneous contractions of the colon. It specifically antagonizes muscarinic receptors. Mepenzolate is marketed under the brand name CANTIL. CANTIL is indicated 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.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
2.6 nM [Ki]
0.68 nM [Ki]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
CANTIL

Doses

AEs

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer


Drug as perpetrator​

Drug as victim

Sourcing

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
The usual adult dose is 1 or 2 tablets (25 or 50 mg) 4 times a day preferably with meals and at bedtime.
Route of Administration: Oral
In Vitro Use Guide
Mepenzolate (10(-8)-10(-5) M), a specific muscarinic receptor antagonist, antagonized contractions of the longitudinal muscle of the isolated guinea-pig ileum preparation elicited by the aqueous extracts of Mareya micrantha suggesting that the cholinergic ingredient(s) in the extract are acting at the muscarinic receptors of the preparation.