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

Study · animal · The American journal of physiology · 1986 · DOI 10.1152/ajpgi.1986.250.4.G553 · PMID 2421587

Plain-language summary

Paraphrased from the published abstract below — not a verdict on whether anything works.

In this in vitro study using rat exocrine pancreas and a colonic tumor cell line, the authors tested a compound predicted from structure-activity studies of rat growth hormone-releasing factor: [4Cl-D-Phe6, Leu17]VIP. They report it competitively antagonized VIP-stimulated amylase release and VIP-stimulated short-circuit current changes, and inhibited amylase release stimulated by rGRF, high concentrations of secretin, and peptide contaminants of a natural glucagon preparation. The abstract reports it did not inhibit the action of agonists for the secretin, GRF, or glucagon receptors.

Abstract

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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