| Autor: |
Wood, M. R., Kim, J. J., Han, W., Dorsey, B. D., Homnick, C. F., DiPardo, R. M., Kuduk, S. D., MacNeil, T., Murphy, K. L., Lis, E. V., Ransom, R. W., Stump, G. L., Lynch, J. J., O'Malley, S. S., Miller, P. J., Chen, T.-B., Harrell, C. M., Chang, R. S. L., Sandhu, P., Ellis, J. D., Bondiskey, P. J., Pettibone, D. J., Freidinger, R. M., Bock, M. G. |
| Zdroj: |
Journal of Medicinal Chemistry; May 2003, Vol. 46 Issue: 10 p1803-1806, 4p |
| Abstrakt: |
Antagonism of the bradykinin B1 receptor was demonstrated to be a potential treatment for chronic pain and inflammation. Novel benzodiazepines were designed that display subnanomolar affinity for the bradykinin B1 receptor (Ki = 0.59 nM) and high selectivity against the bradykinin B2 receptor (Ki > 10 μM). In vivo efficacy, comparable to morphine, was demonstrated for lead compounds in a rodent hyperalgesia model. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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