| Bioactivity | 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. | ||||||||||||
| Target | Ki: 4.6 nM (GABAA α5β3γ2a), 174 nM (GABAA α1β3γ2a), 185 nM (GABAA α2β3γ2a), 80 nM (GABAA α3β3γ2a) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | RO 4938581 | ||||||||||||
| CAS | 883093-10-5 | ||||||||||||
| Formula | C13H8BrF2N5 | ||||||||||||
| Molar Mass | 352.14 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |