RO 4938581 |
カタログ番号GC31238 |
RO 4938581 は強力かつ選択的な GABAA α5 インバース アゴニストであり、GABAA α5β3γ2a に対する Ki は 4.6 nM であり、α1β3γ2a、α2β3γ2a、α3β3γ2a (それぞれ Ki、174、185、80 nM) でより低い親和性を示します。 RO 4938581 は、認知機能障害の研究に使用されています。
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Cas No.: 883093-10-5
Sample solution is provided at 25 µL, 10mM.
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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