| Identification | Back Directory | [Name]
MRK-623 | [CAS]
461449-78-5 | [Synonyms]
MRK-623
Imidazo[1,2-a]pyrimidine-7-methanol, 3-[4-fluoro-3-(3-pyridinyl)phenyl]-α,α-dimethyl- | [Molecular Formula]
C20H17FN4O | [MOL File]
461449-78-5.mol | [Molecular Weight]
348.38 |
| Hazard Information | Back Directory | [Uses]
MRK-623 (Compound 14k) is an orally active, high-affinity GABAA receptor agonist, with the Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect[1]. | [in vivo]
MRK-623 (oral gavage; 0.3, 1, and 3 mg/kg; once) shows anxiolytic effects in the rat elevated plus maze assay[1]. | Animal Model: | Rat | | Dosage: | 0.3, 1, and 3 mg/kg | | Administration: | Oral gavage; 0.3, 1, and 3 mg/kg; once | | Result: | Showed 78% BZ site occupancy at 3 mg/kg, with an ID50 of 0.8 mg/kg. |
| [References]
[1] Simon C Goodacre, et al. Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders. J Med Chem. 2006 Jan 12;49(1):35-8. DOI:10.1021/jm051065l |
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