883093-10-5

883093-10-5 structure

Name: RO 4938581
Chemical Name: RO4938581
CAS Number: 883093-10-5
Molecular Formula: C₁₃H₈BrF₂N₅
Molecular Weight: 352.137
Catalog: Signaling Pathways Membrane Transporter/Ion Channel GABA Receptor
Create Date: 2018-06-27 20:52:42
Modify Date: 2024-01-29 06:48:27
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.

Name	RO4938581
Synonyms	9H-Imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine, 3-bromo-10-(difluoromethyl)- MFCD28133556 RO4938581 3-Bromo-10-(difluoromethyl)-9H-imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine RO 4938581

Description	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.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor Signaling Pathways >> Neuronal Signaling >> GABA Receptor Research Areas >> Neurological Disease
Target	Ki: 4.6 nM (GABAA α5β3γ2a), 174 nM (GABAA α1β3γ2a), 185 nM (GABAA α2β3γ2a), 80 nM (GABAA α3β3γ2a)[1]
In Vitro	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].
In Vivo	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].
References	[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.