Vasoactive intestinal peptide receptor antagonist [4Cl-D-Phe6, Leu17] VIP
- 1 April 1986
- journal article
- research article
- Published by American Physiological Society in American Journal of Physiology-Gastrointestinal and Liver Physiology
- Vol. 250 (4) , G553-G557
- https://doi.org/10.1152/ajpgi.1986.250.4.g553
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.This publication has 9 references indexed in Scilit:
- Receptor for calcitonin gene-related peptide: binding to exocrine pancreas mediates biological actionsAmerican Journal of Physiology-Gastrointestinal and Liver Physiology, 1985
- Interaction of Growth Hormone-Releasing Factor (GRF) and 14 GRF Analogs with Vasoactive Intestinal Peptide (VIP) Receptors of Rat Pancreas. Discovery of (N-Ac-Tyr1,D-Phe2)-GRF(l-29)-NH2as a VIP Antagonist*Endocrinology, 1985
- Vasoactive intestinal polypeptide-induced chloride secretion by a colonic epithelial cell line. Direct participation of a basolaterally localized Na+,K+,Cl- cotransport system.Journal of Clinical Investigation, 1985
- Action of natural glucagon on pancreatic acini: due to contamination by previously undescribed secretagoguesAmerican Journal of Physiology-Gastrointestinal and Liver Physiology, 1983
- Use of 125I-secretin to identify and characterize high-affinity secretin receptors on pancreatic aciniAmerican Journal of Physiology-Gastrointestinal and Liver Physiology, 1983
- Mechanism of [Tyr4]bombesin-induced desensitization in dispersed acini from guinea pig pancreas.Journal of Biological Chemistry, 1982
- Evidence against cyclic GMP as a mediator of the actions of secretagogues on amylase release from guinea-pig pancreasBiochimica et Biophysica Acta (BBA) - General Subjects, 1980
- Kinetics of amylase release by dispersed acini prepared from guinea pig pancreas.American Journal of Physiology-Endocrinology and Metabolism, 1978
- Regulation of amylase release from dispersed pancreatic acinar cells.The Journal of Physiology, 1977