103373-35-9Relevant academic research and scientific papers
Methods for Drug Discovery: Development of Potent, Selective, Orally Effecive Cholecystokinin Antagonists
Evans, B. E.,Rittle, K. E.,Bock, M. G.,DiPardo, R. M.,Freidinger, R. M.,et al.
, p. 2235 - 2246 (2007/10/02)
3-(Acylamino)-5-phenyl-2H-1,4-benzodiazepines, antagonists of the peptide hormone cholecystokinin (CCK), are described.Developed by reasoned modification of the known anxiolytic benzodiazepines, these compounds provide highly potent, orally effective ligands selective for peripheral (CCK-A) receptors, with binding affinities approaching or equaling that of the natural ligand CCK-8.The distinction between CCK-A receptors on the one hand and CNS (CCK-B), gastrin, and central benzodiazepine receptors on the other is demonstrated by using the structure-activity profiles of the new compounds.Details of the binding of these agents to CCK-A receptors are examined, and the method of development of these compounds is discussed in terms of its relevance to the general problem of drug discovery.
