MRK-898

Names

[ CAS No. ]:
461450-30-6

[ Name ]:
MRK-898

Biological Activity

[Description]:

MRK-898 is an orally active GABA(A) receptor modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with Ki values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s)[1].

[Related Catalog]:

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

[Target]

α1 GABA(A) receptor:1.2 nM (Ki)

α2 GABA(A) receptor:1.0 nM (Ki)

α3 GABA(A) receptor:0.73 nM (Ki)

α5 GABA(A) receptor:0.50 nM (Ki)


[References]

[1]. Atack JR. GABAA receptor subtype-selective modulators. I. α2/α3-selective agonists as non-sedating anxiolytics. Curr Top Med Chem. 2011;11(9):1176-202.  

Chemical & Physical Properties

[ Molecular Formula ]:
C20H9F5N4

[ Molecular Weight ]:
400.30

Related Compounds

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