Synthesis of Z-CCK-27-32-NH2, Z-Tyr(SO-3)-Met-Gly-Trp-Met-Asp-NH2, a cholecystokinin receptor antagonist and an inhibitor of gastrin-induced acid secretion.
The synthesis of the hexapeptide Z-Tyr(SO-3)-Met-Gly-Trp-Met-Asp-NH2, representing the C-terminal sequence of cholecystokinin minus the C-terminal phenylalanyl residue is described. This peptide was shown to be the most potent cholecystokinin receptor antagonist in vitro described to date. It is also able to inhibit gastrin-induced acid secretion in vivo, in the rat and was proved to antagonize the action of the C-terminal octapeptide of cholecystokinin in the central nervous system.
D000818:Animals; D002766:Cholecystokinin / Q000138:chemical synthesis* / Q000378:metabolism* / Q000494:pharmacology / Q000031:analogs & derivatives; D005744:Gastric Acid / Q000378:metabolism*; D005750:Gastric Juice / Q000187:drug effects; D005755:Gastrins / Q000494:pharmacology*; D007202:Indicators and Reagents; D009904:Optical Rotation; D010446:Peptide Fragments / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011956:Receptors, Cell Surface / Q000187:drug effects*; D011949:Receptors, Cholecystokinin
D005755:Gastrins; D007202:Indicators and Reagents; D010446:Peptide Fragments; D011956:Receptors, Cell Surface; D011949:Receptors, Cholecystokinin; C038242:cholecystokinin (27-32)-amide; D002766:Cholecystokinin