Ameriks, Michael K. published the artcilePreclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one P2X7 receptor antagonists, Category: chlorides-buliding-blocks, the main research area is dihydrotriazolopyrazinone P2X7 receptor antagonist SAR preparation; 6,7-Dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one; Autoradiography; CNS; Depression; P2X7.
The synthesis, SAR, and preclin. characterization of a series of substituted 6,7-dihydro[1,2,4]triazolo[4,3]pyrazin-8(5H)-one P2X7 receptor antagonists are described. Optimized leads from this series comprise some of the most potent human P2X7R antagonists reported to date (IC50s < 1 nM). They also exhibit sufficient potency and oral bioavailability in rat to enable extensive in vivo profiling. Although many of the disclosed compounds are peripherally restricted, compound I is brain penetrant and upon oral administration demonstrated dose-dependent target engagement in rat hippocampus as determined by ex vivo receptor occupancy with radiotracer II (ED50 = 0.8 mg/kg). Bioorganic & Medicinal Chemistry Letters published new progress about Homo sapiens. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Category: chlorides-buliding-blocks.
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