RO4938581是一种有效的，选择性的GABAAα5反向激动剂，对GABAAα5β3γ2a的Ki值为4.6nM，对α1β3γ2a，α2β3γ2a，α3β3γ2a的亲和性相对较低，Ki值分别为174，185和80nM；RO4938581可用于认知功能障碍的研究。
RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.
RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively)[1].
RO 4938581 (0.3-1 mg/kg, p.o.) reverses a working memory impairment induced by scopolamine the delayed match to position (DMTP) task and a spatial learning impairment induced by diazepam (RO 4938581; 1-10 mg/kg, po)[1].
[1]. Knust H, et al. The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5940-4.
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