Vasoactive intestinal peptide receptor antagonist [4Cl-D-Phe6, Leu17] VIP.
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.
S J
SJ
Pandol
K
K
Dharmsathaphorn
M S
MS
Schoeffield
W
W
Vale
J
J
Rivier
D000681:Amylases / Q000378:metabolism; D000818:Animals; D001839:Bombesin / Q000494:pharmacology; D015740:Calcitonin Gene-Related Peptide; D002217:Carbachol / Q000494:pharmacology; D000242:Cyclic AMP / Q000378:metabolism; D005934:Glucagon / Q000494:pharmacology; D006168:Guinea Pigs; D009419:Nerve Tissue Proteins / Q000494:pharmacology; D010179:Pancreas / Q000378:metabolism; D011956:Receptors, Cell Surface / Q000378:metabolism*; D018005:Receptors, Vasoactive Intestinal Peptide; D012633:Secretin / Q000494:pharmacology; D012844:Sincalide / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013373:Substance P / Q000494:pharmacology; D014660:Vasoactive Intestinal Peptide / Q000031:analogs & derivatives* / Q000494:pharmacology
D009419:Nerve Tissue Proteins; D011956:Receptors, Cell Surface; D018005:Receptors, Vasoactive Intestinal Peptide; C048507:vasoactive intestinal peptide, 4-chloro-Phe(6)-Leu(17)-; D012633:Secretin; D013373:Substance P; D014660:Vasoactive Intestinal Peptide; D002217:Carbachol; D005934:Glucagon; D000242:Cyclic AMP; D000681:Amylases; D015740:Calcitonin Gene-Related Peptide; D012844:Sincalide; D001839:Bombesin