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RO 4938581

Katalog-Nr.GC31238

RO 4938581 ist ein potenter und selektiver inverser Agonist von GABAA α5 mit einem Ki von 4,6 nM fÜr GABAA α5β3γ2a und zeigt eine geringere AffinitÄt zu α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185 bzw. 80 nM); RO 4938581 wird in der Erforschung der kognitiven Dysfunktion verwendet.

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RO 4938581 Chemische Struktur

Cas No.: 883093-10-5

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

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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