DT-Web

DB04843 - Mepenzolate


Identification
Name Mepenzolate
Accession Number DB04843
Type small molecule
Description Mepenzolate is a post-ganglionic parasympathetic inhibitor. It decreases gastric acid and pepsin secretion and suppresses spontaneous contractions of the colon. Mepenzolate diminishes gastric acid and pepsin secretion. Mepenzolate also suppresses spontaneous contractions of the colon. Pharmacologically, it is a post-ganglionic parasympathetic inhibitor. It has not been shown to be effective in contributing to the healing of peptic ulcer, decreasing the rate of recurrence, or preventing complications.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 340.436
Groups approved
Monoisotopic Weight 340.191268703
Pharmacology
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.
Mechanism of action Mepenzolate is a post-ganglionic parasympathetic inhibitor. It specifically antagonizes muscarinic receptors. This leads to decreases in gastric acid and pepsin secretion and suppression of spontaneous contractions of the colon.
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.
Protein binding Not Available
Biotransformation Not Available
Route of elimination 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.
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.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia
Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Mepenzolate, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
Trimethobenzamide Trimethobenzamide and Mepenzolate, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine Triprolidine and Mepenzolate, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Trospium Trospium and Mepenzolate, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Food Interactions Not Available

Targets


Muscarinic acetylcholine receptor M1
Name Muscarinic acetylcholine receptor M1
Gene Name CHRM1
Pharmacological action yes
Actions antagonist
References
  • Tsai CS, Guede-Guina F, Smith MO, Vangah-Manda M, Ochillo RF: Isolation of cholinergic active ingredients in aqueous extracts of Mareya micrantha using the longitudinal muscle of isolated guinea-pig ileum as a pharmacological activity marker. J Ethnopharmacol. 1995 Mar;45(3):215-22. - Pubmed
  • Tsai CS, Ochillo RF: Low temperature and muscarinic receptor activities. Cryobiology. 1989 Oct;26(5):485-95. - Pubmed
  • Ochillo RF, Pugh DA: Atropine and mepenzolate mydriasis in rabbits: a comparative pupillographic analysis of two antimuscarinic agents. Res Commun Chem Pathol Pharmacol. 1982 Jun;36(3):503-6. - Pubmed
DTHybrid score 0.5139
Muscarinic acetylcholine receptor M3
Name Muscarinic acetylcholine receptor M3
Gene Name CHRM3
Pharmacological action yes
Actions antagonist
References
  • Tsai CS, Guede-Guina F, Smith MO, Vangah-Manda M, Ochillo RF: Isolation of cholinergic active ingredients in aqueous extracts of Mareya micrantha using the longitudinal muscle of isolated guinea-pig ileum as a pharmacological activity marker. J Ethnopharmacol. 1995 Mar;45(3):215-22. - Pubmed
  • Tsai CS, Ochillo RF: Low temperature and muscarinic receptor activities. Cryobiology. 1989 Oct;26(5):485-95. - Pubmed
  • Ochillo RF, Pugh DA: Atropine and mepenzolate mydriasis in rabbits: a comparative pupillographic analysis of two antimuscarinic agents. Res Commun Chem Pathol Pharmacol. 1982 Jun;36(3):503-6. - Pubmed
DTHybrid score 0.3877

Predictions


Id Partner name Gene Name Score
617 Muscarinic acetylcholine receptor M2 CHRM2 0.2726
450 Muscarinic acetylcholine receptor M4 CHRM4 0.1663
274 Muscarinic acetylcholine receptor M5 CHRM5 0.1285
4119 Cytochrome P450 2D6 CYP2D6 0.0641
492 Histamine H1 receptor HRH1 0.0583
4512 Cytochrome P450 3A4 CYP3A4 0.0489
3923 Cholinesterase BCHE 0.0382
502 5-hydroxytryptamine 2A receptor HTR2A 0.038
831 D(2) dopamine receptor DRD2 0.031
556 Alpha-1A adrenergic receptor ADRA1A 0.0301
1588 Multidrug resistance protein 1 ABCB1 0.0296
590 5-hydroxytryptamine 2C receptor HTR2C 0.0265
813 Neuronal acetylcholine receptor subunit alpha-2 CHRNA2 0.0253
23 D(1A) dopamine receptor DRD1 0.0229
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0206
6016 Cytochrome P450 2C19 CYP2C19 0.0199
824 Sodium-dependent serotonin transporter SLC6A4 0.0193
4757 Cytochrome P450 2C9 CYP2C9 0.0176
4200 Cytochrome P450 1A2 CYP1A2 0.0176
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0167
789 Alpha-1D adrenergic receptor ADRA1D 0.0165
6013 Cytochrome P450 2E1 CYP2E1 0.0162
632 Alpha-1B adrenergic receptor ADRA1B 0.0153
833 Organic cation/carnitine transporter 1 SLC22A4 0.0144
320 5-hydroxytryptamine 1A receptor HTR1A 0.014
432 D(4) dopamine receptor DRD4 0.0138
6030 Cytochrome P450 2B6 CYP2B6 0.0137
4924 Cytochrome P450 2C8 CYP2C8 0.0133
5878 Alpha-7 nicotinic cholinergic receptor subunit CHRFAM7A 0.0128
4118 Cytochrome P450 3A5 CYP3A5 0.0125
124 Histamine H2 receptor HRH2 0.0123
6104 Dimethylaniline monooxygenase [N-oxide-forming] 1 FMO1 0.012
118 Organic cation/carnitine transporter 2 SLC22A5 0.0113
638 D(3) dopamine receptor DRD3 0.0113
318 Alpha-2A adrenergic receptor ADRA2A 0.0111
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.0103
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.0103
6144 Solute carrier family 22 member 2 SLC22A2 0.0102
2129 Sucrase-isomaltase, intestinal SI 0.0098
436 5-hydroxytryptamine 2B receptor HTR2B 0.0098
378 Alpha-2C adrenergic receptor ADRA2C 0.0096
629 Alpha-2B adrenergic receptor ADRA2B 0.0095
458 Neuronal acetylcholine receptor subunit alpha-10 CHRNA10 0.009
6145 Solute carrier family 22 member 1 SLC22A1 0.0089
1656 CYP2B protein CYP2B 0.0087
528 5-hydroxytryptamine 1E receptor HTR1E 0.0086
713 Sodium-dependent dopamine transporter SLC6A3 0.0082
1256 5-hydroxytryptamine 6 receptor HTR6 0.008
163 D(1B) dopamine receptor DRD5 0.0078
5718 Cytochrome P450 2A6 CYP2A6 0.0076
716 5-hydroxytryptamine 7 receptor HTR7 0.0073
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.007
341 5-hydroxytryptamine 3 receptor HTR3A 0.0069
6107 Cytochrome P450 3A7 CYP3A7 0.0065
725 5-hydroxytryptamine 1D receptor HTR1D 0.0064
885 5-hydroxytryptamine 1B receptor HTR1B 0.0063
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0061
723 Cytosolic phospholipase A2 PLA2G4A 0.0057
6024 Cytochrome P450 1A1 CYP1A1 0.0056
220 Sodium channel protein type 5 subunit alpha SCN5A 0.0053
465 Calmodulin CALM1 0.0049
6432 Transporter snf 0.0041
94 5-hydroxytryptamine 4 receptor HTR4 0.0036
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0033
3876 Aromatic-L-amino-acid decarboxylase DDC 0.0033
380 Cytochrome P450 17A1 CYP17A1 0.0032
587 Serum albumin ALB 0.0031
467 Delta-type opioid receptor OPRD1 0.0031
696 Kappa-type opioid receptor OPRK1 0.0031
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0029
6106 Cytochrome P450 2C18 CYP2C18 0.0029
1360 Sphingomyelin phosphodiesterase SMPD1 0.0028
6147 Solute carrier family 22 member 3 SLC22A3 0.0028
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0028
6182 Cytochrome P450 2J2 CYP2J2 0.0028
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0026
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0025
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0025
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0022
215 Sodium channel protein type 11 subunit alpha SCN11A 0.0021
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.002
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.002
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.002
1618 High affinity nerve growth factor receptor NTRK1 0.0019
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0019
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0019
847 Mu-type opioid receptor OPRM1 0.0018
3941 Amine oxidase [flavin-containing] A MAOA 0.0018
164 Histamine H4 receptor HRH4 0.0017
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0017
474 Acetylcholinesterase ACHE 0.0016
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0015
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0015
20 Prostaglandin G/H synthase 1 PTGS1 0.0015
198 Sodium channel protein type 10 subunit alpha SCN10A 0.0014
193 Beta-1 adrenergic receptor ADRB1 0.0013
766 Beta-2 adrenergic receptor ADRB2 0.0013
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0013
1898 Cytochrome P450 1B1 CYP1B1 0.001
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