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General pharmacology of the four gastrointestinal motility stimulants bethanechol, metoclopramide, trimebutine, and cisapride.
Arzneimittelforschung 1991; 41(6):631-4A

Abstract

The pharmacological profile of bethanechol (CAS 674-38-4), metoclopramide (CAS 364-62-5), trimebutine (CAS 39133-31-8) and cisapride (CAS 81098-60-4) was studied in a series of simple pharmacological tests in rats and dogs. Bethanechol stimulated both gastric emptying and intestinal propulsion but displayed also the well-known behavioral effects of a direct muscarinic acetylcholine receptor agonist. Metoclopramide showed the profile of a centrally active dopamine D2 antagonist. In addition, metoclopramide displayed a stimulant effect on spontaneous gastric emptying in rats, an effect that could not be related to dopamine D2 antagonism. The only effect observed with trimebutine was protection from castor oil diarrhea, probably due to its reported interaction with peripheral opiate receptors. Cisapride was a potent stimulant of gastric emptying in rats, 7 times more potent than metoclopramide. Cisapride was also a very specific gastrokinetic, over a large dose range (specificity ratio: greater than or equal to 20) devoid of effects indicative for direct interaction with dopamine or acetylcholine receptors. The relationship between the differential activity profiles of the compounds in the present study and differences in their mechanism of action and side-effect liability is discussed.

Authors+Show Affiliations

Department of Pharmacology, Janssen Research Foundation, Beerse, Belgium.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

1930352

Citation

Megens, A A., et al. "General Pharmacology of the Four Gastrointestinal Motility Stimulants Bethanechol, Metoclopramide, Trimebutine, and Cisapride." Arzneimittel-Forschung, vol. 41, no. 6, 1991, pp. 631-4.
Megens AA, Awouters FH, Niemegeers CJ. General pharmacology of the four gastrointestinal motility stimulants bethanechol, metoclopramide, trimebutine, and cisapride. Arzneimittelforschung. 1991;41(6):631-4.
Megens, A. A., Awouters, F. H., & Niemegeers, C. J. (1991). General pharmacology of the four gastrointestinal motility stimulants bethanechol, metoclopramide, trimebutine, and cisapride. Arzneimittel-Forschung, 41(6), pp. 631-4.
Megens AA, Awouters FH, Niemegeers CJ. General Pharmacology of the Four Gastrointestinal Motility Stimulants Bethanechol, Metoclopramide, Trimebutine, and Cisapride. Arzneimittelforschung. 1991;41(6):631-4. PubMed PMID: 1930352.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - General pharmacology of the four gastrointestinal motility stimulants bethanechol, metoclopramide, trimebutine, and cisapride. AU - Megens,A A, AU - Awouters,F H, AU - Niemegeers,C J, PY - 1991/6/1/pubmed PY - 1991/6/1/medline PY - 1991/6/1/entrez SP - 631 EP - 4 JF - Arzneimittel-Forschung JO - Arzneimittelforschung VL - 41 IS - 6 N2 - The pharmacological profile of bethanechol (CAS 674-38-4), metoclopramide (CAS 364-62-5), trimebutine (CAS 39133-31-8) and cisapride (CAS 81098-60-4) was studied in a series of simple pharmacological tests in rats and dogs. Bethanechol stimulated both gastric emptying and intestinal propulsion but displayed also the well-known behavioral effects of a direct muscarinic acetylcholine receptor agonist. Metoclopramide showed the profile of a centrally active dopamine D2 antagonist. In addition, metoclopramide displayed a stimulant effect on spontaneous gastric emptying in rats, an effect that could not be related to dopamine D2 antagonism. The only effect observed with trimebutine was protection from castor oil diarrhea, probably due to its reported interaction with peripheral opiate receptors. Cisapride was a potent stimulant of gastric emptying in rats, 7 times more potent than metoclopramide. Cisapride was also a very specific gastrokinetic, over a large dose range (specificity ratio: greater than or equal to 20) devoid of effects indicative for direct interaction with dopamine or acetylcholine receptors. The relationship between the differential activity profiles of the compounds in the present study and differences in their mechanism of action and side-effect liability is discussed. SN - 0004-4172 UR - https://www.unboundmedicine.com/medline/citation/1930352/General_pharmacology_of_the_four_gastrointestinal_motility_stimulants_bethanechol_metoclopramide_trimebutine_and_cisapride_ DB - PRIME DP - Unbound Medicine ER -