| Autor: |
Willson, T. M., Henke, B. R., Momtahen, T. M., Myers, P. L., Sugg, E. E., Unwalla, R. J., Croom, D. K., Dougherty, R. W., Grizzle, M. K., Johnson, M. F., Queen, K. L., Rimele, T. J., Yingling, J. D., James, M. K. |
| Zdroj: |
Journal of Medicinal Chemistry; July 19, 1996, Vol. 39 Issue: 15 p3030-3034, 5p |
| Abstrakt: |
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. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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