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Am J Physiol Gastrointest Liver Physiol 250: G553-G557, 1986;
0193-1857/86 $5.00
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AJP - Gastrointestinal and Liver Physiology, Vol 250, Issue 4 553-G557, Copyright © 1986 by American Physiological Society


ARTICLES

Vasoactive intestinal peptide receptor antagonist [4Cl-D-Phe6, Leu17] VIP

S. J. Pandol, K. Dharmsathaphorn, M. S. Schoeffield, W. Vale and J. Rivier

From structure-activity relationship studies of rat growth hormone-releasing factor (rGFR) on the vasoactive intestinal peptide (VIP) receptor in an in vitro preparation of exocrine pancreas, we predicted that [4Cl-D-Phe6, Leu17]VIP would be a competitive antagonist for the action of VIP. Micromolar concentrations of synthetic [4Cl-D-Phe6, Leu17]VIP competitively antagonized VIP-stimulated amylase release in the pancreatic preparation and VIP-stimulated short-circuit current changes in a colonic tumor cell line. In addition, [4Cl-D-Phe6, Leu17]VIP inhibited amylase release stimulated by rGRF, high concentrations of secretin (agents that act through the VIP receptor), and peptide contaminants in a preparation of natural glucagon. Finally, [4Cl-D-Phe6, Leu17]VIP did not inhibit the action of agonists for the secretin, GRF, or glucagon receptors.





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