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1987 | OriginalPaper | Chapter

Synthesis and Biological Activity of Agonists for the Neuronal Tachykinin Receptor in Guinea Pig Ileum

Authors : D. Ron, R. Laufer, J. Frey, C. Gilon, Z. Selinger, M. Chorev

Published in: Substance P and Neurokinins

Publisher: Springer New York

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The classification of tachykinin receptors into two subclasses, the SP-P and the SP-E receptors has been well established (1). Recently Laufer et. al. (2) characterized, in the guinea pig ileum, a third tachykinin receptor subclass, designated as SP-N receptor. The SP-N receptor is located on the enteric cholinergic neurons, and madiates the release of acetylcholine. We found that the SP analog (pGlu6,(N-Me)Phe8) SP6-11 acts as a selective potent agonist for the SP-N receptor (EC50=0.5 nM) while its potency for the SP-P receptor is much lower (EC50=500 nM). Conceivably N-methylation of Phe8 in the hexapeptide sequence of substance P (SP), induces selectivity toward the SP-N receptor. Therefore we set to probe the constraints at the nitrogen of Phe7-Phe8 amide bond by changing the alkyl group at this site.

Metadata
Title
Synthesis and Biological Activity of Agonists for the Neuronal Tachykinin Receptor in Guinea Pig Ileum
Authors
D. Ron
R. Laufer
J. Frey
C. Gilon
Z. Selinger
M. Chorev
Copyright Year
1987
Publisher
Springer New York
DOI
https://doi.org/10.1007/978-1-4612-4672-5_48