New glutaramic acid derivatives with potent competitive and specific cholecystokinin-antagonistic activity.
New glutaramic acid derivatives were evaluated for anti-cholecystokinin (CCK) activity in vitro on guinea pig gallbladder. The compounds are competitive and specific CCK-antagonists, causing a parallel right shift of the cumulative dose-response curve of the agonist. The affinity for the binding site of the CCK-receptor for some of these compounds was hundreds of times higher than that of pro-glumide, the model compound.
D000109:Acetylcholine / Q000494:pharmacology; D000818:Animals; D002766:Cholecystokinin / Q000037:antagonists & inhibitors*; D005704:Gallbladder / Q000187:drug effects; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D066298:In Vitro Techniques; D007421:Intestine, Small / Q000187:drug effects; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects*; D011377:Proglumide / Q000494:pharmacology; D011817:Rabbits; D013329:Structure-Activity Relationship
D006632:Histamine; D002766:Cholecystokinin; D011377:Proglumide; D000109:Acetylcholine