ONO-8590580

ONO-8590580

CAT N°: 35297
Price:

From 270.00 229.50

ONO-8590580 is a negative allosteric modulator of ?5 subunit-containing GABAA receptors that binds at the benzodiazepine binding site.{68102} It binds to ?1, ?2, ?3, and ?5 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 ?5?3?2 subunits (EC50 = 1.1 nM) over those expressing human recombinant ?1?3?2, ?2?3?2, or ?3?3?2 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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