一种口服生物可利用的、对GABAAα5受体苯二氮䓬位点具有功能选择性的反向激动剂，具有认知增强特性。
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.
作者信息
Chambers Mark S, Atack John R, Carling Robert W, Collinson Neil, Cook Susan M, Dawson Gerard R, Ferris Pushpindar, Hobbs Sarah C, O'connor Desmond, Marshall George, Rycroft W, Macleod Angus M
机构信息
Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, CM20 2QR, UK.
出版信息
J Med Chem. 2004 Nov 18;47(24):5829-32. doi: 10.1021/jm040863t.
(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 GABA(A) alpha5 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 GABA(A) inverse agonists.
（3-叔丁基-7-（5-甲基异恶唑-3-基）-2-（1-甲基-1H-1,2,4-三唑-5-基甲氧基）吡唑并[1,5-d][1,2,4]三嗪（13）已被确定为GABA(A)α5受体苯二氮䓬位点的功能选择性反向激动剂。13具有口服生物利用度，易于穿透中枢神经系统，并能提高动物认知模型中的表现。它不表现出与非选择性GABA(A)反向激动剂相关的惊厥、促惊厥或致焦虑活性。
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