Autor: |
C. Goodacre, Simon, J. Street, Leslie, J. Hallett, David, M. Crawforth, James, Kelly, Sarah, P. Owens, Andrew, P. Blackaby, Wesley, T. Lewis, Richard, Stanley, Joanna, J. Smith, Alison, Ferris, Pushpinder, Sohal, Bindi, M. Cook, Susan, Pike, Andrew, Brown, Nicola, A. Wafford, Keith, Marshall, George, L. Castro, José, R. Atack, John |
Zdroj: |
Journal of Medicinal Chemistry; January 2006, Vol. 49 Issue: 1 p35-38, 4p |
Abstrakt: |
A series of high-affinity GABAA agonists with good oral bioavailability in rat and dog and functional selectivity for the GABAAα2 and -α3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g and the 7-propan-2-olimidazopyrimidine 14k are anxiolytic in both conditioned and unconditioned animal models of anxiety with minimal sedation observed at full BZ binding site occupancy. |
Databáze: |
Supplemental Index |
Externí odkaz: |
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