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Motor-stimulating properties of cisapride on isolated gastrointestinal preparations of the guinea pig.
J Pharmacol Exp Ther. 1985 Sep; 234(3):775-83.JP

Abstract

The effects of cisapride (R 51619), a new non-dopamine-blocking gastrokinetic drug, on gastrointestinal contractility have been determined on isolated preparations of the guinea pig. On the intact gastroduodenal preparation, cisapride enhanced contractile amplitude (3.4 X 10(-7) M), improved antroduodenal coordination (EC50 = 1.9 X 10(-7) M) and antagonized gastric relaxation induced by phenylephrine, dopamine, isoproterenol, 5-hydroxytryptamine (in the presence of atropine) and periarterial nerve stimulation (IC50 range, 9.1 X 10(-7)-2.4 X 10(-6) M). Experiments with metoclopramide yielded similar results on amplitude, coordination and dopamine-induced relaxation at 5 X 10(-5), 2.2 X 10(-5) and 1.7 X 10(-5) M, respectively. On the ileum, cisapride enhanced the contractile response to electrical stimulation at low concentrations (EC50 = 9.2 X 10(-9) M) as compared with metoclopramide (EC50 = 3.3 X 10(-6) M). On this preparation, cisapride showed no direct cholinergic or nicotine-like effects and did not enhance the response to methacholine (indicative of a lack of inhibition of acetylcholinesterase-activity and of sensitization of the muscarine receptor). On the colon ascendens, cisapride induced contractions (EC50 = 3.5 X 10(-8) M) (metoclopramide, 3.5 X 10(-6) M), insensitive to atropine and only marginally inhibited by tetrodotoxin. In conclusion, cisapride effectively improves spontaneous or electrically evoked contractions of isolated preparations of the guinea pig, most likely via facilitation of the release of acetylcholine. However, the inhibition of gastric relaxation and the induction of colonic contractions in the presence of atropine indicate that, besides cholinergic neuronal pathways, other mechanisms are involved in the motor-stimulating properties of cisapride.

Authors

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Pub Type(s)

Journal Article

Language

eng

PubMed ID

3897516

Citation

Schuurkes, J A., et al. "Motor-stimulating Properties of Cisapride On Isolated Gastrointestinal Preparations of the Guinea Pig." The Journal of Pharmacology and Experimental Therapeutics, vol. 234, no. 3, 1985, pp. 775-83.
Schuurkes JA, Van Nueten JM, Van Daele PG, et al. Motor-stimulating properties of cisapride on isolated gastrointestinal preparations of the guinea pig. J Pharmacol Exp Ther. 1985;234(3):775-83.
Schuurkes, J. A., Van Nueten, J. M., Van Daele, P. G., Reyntjens, A. J., & Janssen, P. A. (1985). Motor-stimulating properties of cisapride on isolated gastrointestinal preparations of the guinea pig. The Journal of Pharmacology and Experimental Therapeutics, 234(3), 775-83.
Schuurkes JA, et al. Motor-stimulating Properties of Cisapride On Isolated Gastrointestinal Preparations of the Guinea Pig. J Pharmacol Exp Ther. 1985;234(3):775-83. PubMed PMID: 3897516.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Motor-stimulating properties of cisapride on isolated gastrointestinal preparations of the guinea pig. AU - Schuurkes,J A, AU - Van Nueten,J M, AU - Van Daele,P G, AU - Reyntjens,A J, AU - Janssen,P A, PY - 1985/9/1/pubmed PY - 1985/9/1/medline PY - 1985/9/1/entrez SP - 775 EP - 83 JF - The Journal of pharmacology and experimental therapeutics JO - J. Pharmacol. Exp. Ther. VL - 234 IS - 3 N2 - The effects of cisapride (R 51619), a new non-dopamine-blocking gastrokinetic drug, on gastrointestinal contractility have been determined on isolated preparations of the guinea pig. On the intact gastroduodenal preparation, cisapride enhanced contractile amplitude (3.4 X 10(-7) M), improved antroduodenal coordination (EC50 = 1.9 X 10(-7) M) and antagonized gastric relaxation induced by phenylephrine, dopamine, isoproterenol, 5-hydroxytryptamine (in the presence of atropine) and periarterial nerve stimulation (IC50 range, 9.1 X 10(-7)-2.4 X 10(-6) M). Experiments with metoclopramide yielded similar results on amplitude, coordination and dopamine-induced relaxation at 5 X 10(-5), 2.2 X 10(-5) and 1.7 X 10(-5) M, respectively. On the ileum, cisapride enhanced the contractile response to electrical stimulation at low concentrations (EC50 = 9.2 X 10(-9) M) as compared with metoclopramide (EC50 = 3.3 X 10(-6) M). On this preparation, cisapride showed no direct cholinergic or nicotine-like effects and did not enhance the response to methacholine (indicative of a lack of inhibition of acetylcholinesterase-activity and of sensitization of the muscarine receptor). On the colon ascendens, cisapride induced contractions (EC50 = 3.5 X 10(-8) M) (metoclopramide, 3.5 X 10(-6) M), insensitive to atropine and only marginally inhibited by tetrodotoxin. In conclusion, cisapride effectively improves spontaneous or electrically evoked contractions of isolated preparations of the guinea pig, most likely via facilitation of the release of acetylcholine. However, the inhibition of gastric relaxation and the induction of colonic contractions in the presence of atropine indicate that, besides cholinergic neuronal pathways, other mechanisms are involved in the motor-stimulating properties of cisapride. SN - 0022-3565 UR - https://www.unboundmedicine.com/medline/citation/3897516/Motor_stimulating_properties_of_cisapride_on_isolated_gastrointestinal_preparations_of_the_guinea_pig_ L2 - http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=3897516 DB - PRIME DP - Unbound Medicine ER -