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N-acylated pentapeptides antagonists of substance P on guinea-pig ileum
P Schmitt1, M Mayer, S Magneney
1Institut de Chimie des Substances Naturelles, CNRS 91198, Gif sur Yvette, France.
Biochemical and Biophysical Research Communications
|October 14, 1988
Abstract:
Pentapeptides X-D.Trp-Phe-D.Trp-Leu-Y-NH2 (X = H, Boc, parahydroxyphenylacetyl, Y = Met,Leu,Nle,Phe) were tested as antagonists against Substance P and against a specific agonist of the muscular receptor of neurokinins on the guinea-pig ileum. Weak antagonist or agonist activities could be observed with the free or the Boc-protected pentapeptides whilst the acylated compounds could be compared favorably with the best antagonists already described.