Cholecystokinin-A receptor ligands based on the. kappa.-opioid agonist tifluadom

MG Bock, RM DiPardo, BE Evans…

文献索引：Bock, Mark G.; DiPardo, Robert M.; Evans, Ben E.; Rittle, Kenneth E.; Whitter, Willie L.; et al. Journal of Medicinal Chemistry, 1990 , vol. 33, # 1 p. 450 - 455

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被引用次数: 22

摘要

Tifluadom, a K-opioid agonist and cholecystokinin-A (CCK-A) receptor antagonist, was utilized as a model to prepare a series of 2-(aminomethy1)-and 3-(aminomethyl)-1, 4- benzodiazepines. These compounds were tested in vitro as inhibitors of the binding of [1261] CCK to rat pancreas and guinea pig brain receptors. All compounds with ICF's less than 100 pM proved to have greater affinity for the CCK-A receptor, with the most potent ...