Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.

@article{Evans1988MethodsFD,
  title={Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.},
  author={B. Evans and K. Rittle and M. Bock and R. M. Dipardo and R. Freidinger and W. L. Whitter and G. F. Lundell and D. Veber and P. S. Anderson and R. Chang},
  journal={Journal of medicinal chemistry},
  year={1988},
  volume={31 12},
  pages={
          2235-46
        }
}
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… Expand
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A series of 3-substituted 5-phenyl-1,4-benzodiazepines, nonpeptidal antagonists of the peptide hormone cholecystokinin, serve to illuminate the distinction between central and peripheral CCK receptors, as well as to provide orally effective CCK antagonists of potential pharmacological or therapeutic utility. Expand
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We describe the design and synthesis of nonpeptidal antagonists of the peptide hormone cholecystokinin. Several of these compounds have high specificity and nanomolar binding affinity and are activeExpand
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