title: Different peripheral and central antagonistic activity of new glutaramic acid derivatives on satiety induced by cholecystokinin in rats.
abstract: New glutaramic acid derivatives with cholecystokinin antagonistic activity were evaluated for their capacity to inhibit the satiety effect induced in the rat by intraperitoneal (i.p.) injection of cholecystokinin octapeptide (CCK-8). The most active compound, CR 1409, is about 4000 times more potent than proglumide when injected peripherally (i.p.). This compound competitively inhibits the action of CCK-8 at the receptor responsible for the satiety effect. In contrast, CR 1409, i.p. or intracerebroventricularly (i.c.v.) injected does not exhibit antagonistic effects when CCK-8 is administered i.c.v., confirming the existence of at least two different populations of CCK receptors.
mesh_terms: D000818:Animals; D004305:Dose-Response Relationship, Drug; D005973:Glutamine / Q000031:analogs & derivatives*; D008297:Male; D011377:Proglumide / Q000031:analogs & derivatives* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011949:Receptors, Cholecystokinin / Q000032:analysis / Q000502:physiology; D012527:Satiation / Q000187:drug effects*; D012844:Sincalide / Q000037:antagonists & inhibitors*
chemical_list: D011949:Receptors, Cholecystokinin; D005973:Glutamine; D011377:Proglumide; C048181:lorglumide; D012844:Sincalide