RO 4938581 |
Catalog No.GC31238 |
RO 4938581은 GABAA α5β3γ2a에 대해 Ki가 4.6nM인 강력하고 선택적인 GABAA α5 역작용제이며 α1β3γ2a, α2β3γ2a, α3β3γ2a(각각 Ki, 174), 185에서 더 낮은 친화도를 나타냅니다. RO 4938581은 인지 기능 장애 연구에 사용됩니다.
Products are for research use only. Not for human use. We do not sell to patients.
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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