1025841-36-4Relevant academic research and scientific papers
Improving the Affinity and Selectivity of a Nonpeptide Series of Cholecystokinin-B/Gastrin Receptor Antagonists Based on the Dibenzobicyclooctane Skeleton
Kalindjian, S. Barret,Buck, Ildiko M.,Cushnir, Julia R.,Dunstone, David J.,Hudson, Martin L.,et al.
, p. 4294 - 4302 (2007/10/03)
We have recently described a novel series of nonpeptidic cholecystokinin-B (CCKB)/gastrin receptor antagonists based on a dibenzobicyclooctane skeleton.We wish now to report on compounds arising out of our earlier work which have substantially greater affinity as antagonists for the CCKB/gastrin receptor system and which maintain, or improve on, the already high selectivity with respect to CCKA receptors.Thus, cis-7-carbonyl>-2-phenylethyl>amino>carbonyl>-8--carbonyl>-2,3:5,6-dibenzobicycloi of 8.80 in mouse cortical membranes at CCKB/gastrin receptors.THe selectivity for these receptors over CCKA receptors was in the order of 1000-fold.
