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See Latest ArticlesIn vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)-pyrazolo[1,5-d][1,2,4]triazine (MRK-016), a GABAA receptor alpha 5 subtype-selective inverse agonist
Journal of Pharmacology and Experimental Therapeutics, 08/25/09
Atack JR et al. – In man MRK–016 had a longer half–life than in preclinical species and although it was well tolerated in young males, with a maximal tolerated single dose of 5 mg corresponding to an estimated occupancy in the region of 75%, MRK–016 was poorly tolerated in elderly subjects, even at a dose of 0.5 mg, which, along with its variable human pharmacokinetics, precluded its further development.
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