| Literature DB >> 8709137 |
T M Willson1, B R Henke, T M Momtahen, P L Myers, E E Sugg, R J Unwalla, D K Croom, R W Dougherty, M K Grizzle, M F Johnson, K L Queen, T J Rimele, J D Yingling, M K James.
Abstract
A series of modifications were made to the C-3 substituent of the 1,5-benzodiazepine CCK-A agonist 1. Replacement of the inner urea NH and addition of a methyl group to generate a C-3 quaternary carbon resulted in acetamide 6, which showed CCK-A receptor binding selectivity and sub-micromolar agonist activity in vitro. Benzodiazepine 6 was active in an in vivo mouse gallbladder emptying assay and represents a novel orally active, binding selective CCK-A agonist.Entities:
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Year: 1996 PMID： 8709137 DOI： 10.1021/jm960205b
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446