GABAA receptor modulator-2

Names

[ CAS No. ]:
2413850-54-9

[ Name ]:
GABAA receptor modulator-2

Biological Activity

[Description]:

GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABAAR negative allosteric modulator (NAM) with a Ki of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[Target]

Ki: 4.1 nM (hα5)[1]


[In Vivo]

GABAA receptor modulator-2 (Compound 20) (0-10 mg/kg) produces a dose-dependent reversal of the PCP-induced cognitive deficit in the rat subPCP NOR test[1].

[References]

[1]. Szabó G, et al. Multiparameter Optimization of Naphthyridine Derivatives as Selective α5-GABAA Receptor Negative Allosteric Modulators. J Med Chem. 2022 Jun 9;65(11):7876-7895.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H22FN3O5S

[ Molecular Weight ]:
459.49

Related Compounds