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Science 23 November 1984:
Vol. 226. no. 4677, pp. 987 - 989
DOI: 10.1126/science.6095447
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Articles

Science, Vol 226, Issue 4677, 987-989
Copyright © 1984 by American Association for the Advancement of Science

articles

Novel pharmacology of substance K-binding sites: a third type of tachykinin receptor

SH Buck, E Burcher, CW Shults, W Lovenberg, and TL O'Donohue

The tachykinins are a family of peptides with the carboxyl terminal amino acid sequence Phe-X-Gly-Leu-Met-NH2. Three major mammalian tachykinins have been identified--substance K, neuromedin K, and substance P--but only two tachykinin receptors have been postulated. Three tachykinins were labeled with radioiodinated Bolton-Hunter reagent and their binding characteristics were determined in crude membrane suspensions from several tissues. In cerebral cortex labeled eledoisin exhibited high-affinity binding that was inhibited by tachykinins in a manner indicating a definitive SP-E receptor site. In gastrointestinal smooth muscle and bladder, high-affinity binding of labeled substance P was inhibited in a pattern indicating a definitive SP-P site. In intestinal smooth muscle and bladder, however, labeled substance K and labeled eledoisin were both bound in a pattern indicating a preference for substance K itself. The results suggest the existence of three distinct types of tachykinin receptors: SP-P, SP-E, and SP-K.


THIS ARTICLE HAS BEEN CITED BY OTHER ARTICLES:
Pharmacokinetics of the Bicyclic Peptide Tachykinin NK2 Receptor Antagonist MEN 11420 (Nepadutant) in Rats.
A. Lippi, M. Criscuoli, M. Guelfi, P. Santicioli, and C. A. Maggi (1998)
Drug Metab. Dispos. 26, 1077-1081
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Neurokinin A increases duodenal mucosal permeability, bicarbonate secretion, and fluid output in the rat.
A. Hallgren, G. Flemstrom, P. M. Hellstrom, M. Lordal, S. Hellgren, and O. Nylander (1997)
Am J Physiol Gastrointest Liver Physiol 273, G1077-G1086
   Abstract »    Full Text »    PDF »
Effects of Substance P and Substance P Antagonists on Rat Salivary Secretion.
E. Bobyock, E.J. Barbieri, and W.S. Chernick (1986)
Journal of Dental Research 65, 1427-1431
   Abstract »    PDF »


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