Formulation: A solid
Formal Name: 3-(1,1-dimethylethyl)-7-(5-methyl-3-isoxazolyl)-2-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-pyrazolo[1,5-d][1,2,4]triazine
Purity: ≥98%
Formula Markup: C17H20N8O2
Formula Weight: 368,4
Shelf life (days): 1460
CAS Number: 342652-67-9
Notes: MRK-016 is a functionally selective inverse agonist of α5 subunit-containing GABAA receptors.{65493} It selectively binds to α1-, α2-, α3-, and α5 subunit-containing GABAA receptors (Kis = 0.83, 0.85, 0.77, and 1.4 nM, respectively) over those containing α4 or α6 subunits (Kis = 395 and >4,000 nM, respectively). It also selectively inhibits GABA-induced currents in mouse fibroblast L-M(TK-) cells expressing α5 subunit-containing GABAA receptors over those containing α1, α2, or α3 subunits. MRK-016 (3 mg/kg) reverses LPS-induced decreases in Bdnf expression, but not LPS-induced increases in amyloid-β levels, in the mouse hippocampus.{65494} It reverses LPS-induced inhibition of contextual fear acquisition in the same study, indicating a reversal of memory consolidation deficits.{65494} It enhances the performance of wild-type rats in a delayed matching-to-place water maze when administered at doses of 0.3, 1, and 3 mg/kg, indicating nootropic properties.{65493} MRK-016 also reduces immobility in the forced swim test in mice, an effect that can be blocked by the AMPA glutamate receptor antagonist NBQX (Item No. 14914).{65495} It does not potentiate proconvulsant activity induced by pentylenetetrazole (Item No. 18682) in mice when administered at doses up to 10 mg/kg.{65493}
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