| Autor: |
Chambers, M. S., Atack, J. R., Carling, R. W., Collinson, N., Cook, S. M., Dawson, G. R., Ferris, P., Hobbs, S. C., O'Connor, D., Marshall, G., Rycroft, W., MacLeod, A. M. |
| Zdroj: |
Journal of Medicinal Chemistry; November 2004, Vol. 47 Issue: 24 p5829-5832, 4p |
| Abstrakt: |
(3-tert-Butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)pyrazolo[1,5-d][1,2,4]triazine (13) has been identified as a functionally selective, inverse agonist at the benzodiazepine site of GABAA α5 receptors. 13 is orally bioavailable, readily penetrates the CNS, and enhances performance in animal models of cognition. It does not exhibit the convulsant, proconvulsant, or anxiogenic activity associated with nonselective GABAA inverse agonists. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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