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ONO-8590580

Chemical Structure : ONO-8590580

CAS No.: 1802661-73-9

ONO-8590580 (ONO8590580, ONO 8590580)

Catalog No.: PC-63442Not For Human Use, Lab Use Only.

ONO-8590580 is a novel potent, selective GABAA α5 negative allosteric modulator, binds to the benzodiazepine binding sites on recombinant human α5-containing GABAA receptors with Ki of 7.9 nM.

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Biological Activity

ONO-8590580 (ONO 8590580) is a novel potent, selective GABAA α5 negative allosteric modulator, binds to the benzodiazepine binding sites on recombinant human α5-containing GABAA receptors with Ki of 7.9 nM.
ONO-8590580 shows functionally selective GABAA α5 NAM activity for GABA-induced Cl- channel activity with a maximum 44.4% inhibition and an EC50 of 1.1 nM.
ONO-8590580 significantly augments tetanus-induced long-term potentiation of CA1 synapse response in rat hippocampal slices at 300 nM.
ONO-8590580 significantly prevents MK-801-induced memory deficit in vivo (3-20 mg/kg, p.o.).

Physicochemical Properties

M.Wt 376.439
Formula C21H21FN6
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(cyclopropylmethyl)-5-fluoro-4-methyl-N-[5-(1-methyl-1H-imidazol-4-yl)-2-pyridinyl]-1H-benzimidazol-6-amine

References

1. Kawaharada S, et al. J Pharmacol Exp Ther. 2018 Apr 19. pii: jpet.117.247627.

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