Benzodiazepines as Potent and Selective Bradykinin B1 Antagonists

التفاصيل البيبلوغرافية
العنوان:	Benzodiazepines as Potent and Selective Bradykinin B1 Antagonists
المؤلفون:	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.
المصدر:	Journal of Medicinal Chemistry; May 2003, Vol. 46 Issue: 10 p1803-1806, 4p
مستخلص:	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.
قاعدة البيانات:	Supplemental Index

الوصف
تدمد:	00222623 15204804