Differentiation of central and peripheral cholecystokinin receptors by new glutaramic acid derivatives with cholecystokinin-antagonistic activity.
Three glutaramic acid derivatives provided with a potent antagonistic activity on the contractions elicited by the carboxyl terminal octapeptide CCK-8 in the guinea pig gallbladder have been evaluated for their capacity to inhibit the binding of [125I]-(Bolton-Hunter)-CCK-8 to both central and peripheric cholecystokinin (CCK) receptors. The most active compound inhibits the CCK binding to rat pancreas acini at a concentration 10(-7) mol/l, but only at 10(-4) mol/l on cerebral cortex membranes, confirming the existence of at least two different populations of CCK receptors.
D000818:Animals; D001549:Benzamides / Q000494:pharmacology; D002540:Cerebral Cortex / Q000378:metabolism*; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D051379:Mice; D010179:Pancreas / Q000378:metabolism*; D011377:Proglumide / Q000031:analogs & derivatives / Q000494:pharmacology; D051381:Rats; D011956:Receptors, Cell Surface / Q000187:drug effects / Q000378:metabolism*; D011949:Receptors, Cholecystokinin; D012844:Sincalide / Q000378:metabolism; D013758:Tetragastrin / Q000494:pharmacology
D001549:Benzamides; D011956:Receptors, Cell Surface; D011949:Receptors, Cholecystokinin; D013758:Tetragastrin; C048182:CR 1372; C048183:CR 1392; D011377:Proglumide; C048181:lorglumide; C013841:benzotript; D012844:Sincalide