| Autor: |
McCauley, J. A., Theberge, C. R., Romano, J. J., Billings, S. B., Anderson, K. D., Claremon, D. A., Freidinger, R. M., Bednar, R. A., Mosser, S. D., Gaul, S. L., Connolly, T. M., Condra, C. L., Xia, M., Cunningham, M. E., Bednar, B., Stump, G. L., Lynch, J. J., Macaulay, A., Wafford, K. A., Koblan, K. S., Liverton, N. J. |
| Zdroj: |
Journal of Medicinal Chemistry; April 2004, Vol. 47 Issue: 8 p2089-2096, 8p |
| Abstrakt: |
Two classes of 5-substituted benzimidazoles were identified as potent antagonists of the NR2B subtype of the N-methyl-d-aspartate (NMDA) receptor. Selected compounds show very good selectivity versus the NR2A, NR2C, and NR2D subtypes of the NMDA receptor as well as versus hERG-channel activity and α1-adrenergic binding. Benzimidazole 37a shows excellent activity in the carrageenan-induced mechanical hyperalgesia assay in rats as well as good pharmacokinetic behavior in dogs. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
|
