Formulation: A crystalline solid
Formal Name: 1-(cyclopropylmethyl)-5-fluoro-4-methyl-N-[5-(1-methyl-1H-imidazol-4-yl)-2-pyridinyl]-1H-benzimidazol-6-amine
Purity: ≥98%
Formula Markup: C21H21FN6
Formula Weight: 376,4
Shelf life (days): 1460
CAS Number: 1802661-73-9
Notes: ONO-8590580 is a negative allosteric modulator of α5 subunit-containing GABAA receptors that binds at the benzodiazepine binding site.{68102} It binds to α1, α2, α3, and α5 subunit-containing GABAA receptors (Kis = 140, 32, 24, and 7.9 nM, respectively). It is selective for inhibiting GABA-induced currents in HEK293 cells expressing human recombinant α5β3γ2 subunits (EC50 = 1.1 nM) over those expressing human recombinant α1β3γ2, α2β3γ2, or α3β3γ2 subunits for which it has little to no activity. ONO-8590580 (300 nM) enhances long-term potentiation in rat hippocampal brain slices. It decreases MK-801-induced memory deficits in the rat passive avoidance test when administered at doses ranging from 3 to 20 mg/kg. ONO-8590580 (20 mg/kg, p.o.) decreases MK-801- and scopolamine-induced increases in the latency to complete, and the number of errors made in, the eight-arm radial maze test in rats. It does not induce anxiety-like or proconvulsant behavior in rats in the elevated zero maze or pentylenetetrazole-induced seizure test when administered at a dose of 20 mg/kg.
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