| Autor: |
Zheng, G. Z., Bhatia, P., Daanen, J., Kolasa, T., Patel, M., Latshaw, S., Kouhen, O. F. El, Chang, R., Uchic, M. E., Miller, L., Nakane, M., Lehto, S. G., Honore, M. P., Moreland, R. B., Brioni, J. D., Stewart, A. O. |
| Zdroj: |
Journal of Medicinal Chemistry; November 2005, Vol. 48 Issue: 23 p7374-7388, 15p |
| Abstrakt: |
SAR (structure−activity relationship) studies of triazafluorenone derivatives as potent mGluR1 antagonists are described. The triazafluorenone derivatives are non-amino acid derivatives and noncompetitive mGluR1 antagonists that bind at a putative allosteric recognition site located within the seven-transmembrane domain of the receptor. These triazafluorenone derivatives are potent, selective, and systemically active mGluR1 antagonists. Compound 1n, for example, was a very potent mGluR1 antagonist (IC50 = 3 nM) and demonstrated full efficacy in various in vivo animal pain models. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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