Document Report Card

ID: ALA1134388

Journal: J Med Chem

Title: Nonpeptide cholecystokinin-2 receptor agonists.

Authors: Kalindjian SB, Dunstone DJ, Low CM, Pether MJ, Roberts SP, Tozer MJ, Watt GF, Shankley NP.

Abstract: In the course of structural explorations around a series of potent CCK2 receptor antagonists, it was noted that simple N-methylation of the indolic N-H in the parent molecule gave rise to behavior in vivo that was consistent with the compound acting as an agonist. Exploration in vitro confirmed this property, and it was shown that the agonist action could be blocked by the reference CCK2 receptor antagonist, L-365,260. Further examples of this type of modification were explored, and a common theme with regard to agonist behavior was uncovered. Some molecular modeling is also presented in an attempt to throw light on the nature of the ligand receptor interactions that may be giving rise to the differing properties of these, apparently, structurally similar molecules.

CiteXplore: 11312913

DOI: 10.1021/jm0010668