Abstract
We investigated the influence of the nonpeptide neurotensin receptor antagonist, SR 48692, administered orally, on gastric emptying and on acute defaecation. SR 48692 dose-dependently (ED50 approximately 0.7 microgram kg-1) increased gastric emptying of a food suspension, but it had no effect on that of a non-caloric meal. SR 48692 also dose-dependently promoted defaecation and increased faecal water content. We suggest that antagonism of endogenous neurotensin accounts for the gastric emptying and defaecation promoting action of SR 48692.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Croci T., Bianchetti A. Stimulation of faecal excretion in rats by alpha 2-adrenergic antagonists. J Pharm Pharmacol. 1992 Apr;44(4):358–360. doi: 10.1111/j.2042-7158.1992.tb03621.x. [DOI] [PubMed] [Google Scholar]
- Gully D., Canton M., Boigegrain R., Jeanjean F., Molimard J. C., Poncelet M., Gueudet C., Heaulme M., Leyris R., Brouard A. Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor. Proc Natl Acad Sci U S A. 1993 Jan 1;90(1):65–69. doi: 10.1073/pnas.90.1.65. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Hellström P. M., Nylander G., Rosell S. Effects of neurotensin on the transit of gastrointestinal contents in the rat. Acta Physiol Scand. 1982 Jun;115(2):239–243. doi: 10.1111/j.1748-1716.1982.tb07071.x. [DOI] [PubMed] [Google Scholar]
- Labbé-Jullié C., Deschaintres S., Gully D., Le Fur G., Kitabgi P. Effect of the nonpeptide neurotensin antagonist, SR 48692, and two enantiomeric analogs, SR 48527 and SR 49711, on neurotensin binding and contractile responses in guinea pig ileum and colon. J Pharmacol Exp Ther. 1994 Oct;271(1):267–276. [PubMed] [Google Scholar]
- Vita N., Laurent P., Lefort S., Chalon P., Dumont X., Kaghad M., Gully D., Le Fur G., Ferrara P., Caput D. Cloning and expression of a complementary DNA encoding a high affinity human neurotensin receptor. FEBS Lett. 1993 Feb 8;317(1-2):139–142. doi: 10.1016/0014-5793(93)81509-x. [DOI] [PubMed] [Google Scholar]