| Identification | Back Directory | [Name]
[1,1'-Biphenyl]-2-carbonitrile, 2',4-difluoro-5'-[7-(trifluoromethyl)imidazo[1,2-a]pyrimidin-3-yl]- | [CAS]
461450-30-6 | [Synonyms]
MRK-898
[1,1'-Biphenyl]-2-carbonitrile, 2',4-difluoro-5'-[7-(trifluoromethyl)imidazo[1,2-a]pyrimidin-3-yl]- | [Molecular Formula]
C20H9F5N4 | [MOL File]
461450-30-6.mol | [Molecular Weight]
400.3 |
| Hazard Information | Back Directory | [Uses]
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]. | [IC 50]
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. DOI:10.2174/156802611795371350 |
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