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R4996 is an investigational small-molecule partial agonist of the nicotinic alpha-7 receptor that was developed under a nicotinic receptor collaboration between Memory Pharmaceuticals and Roche for the treatment of cognitive disorders such as Alzheimer’s disease and schizophrenia.[1][4][7] In Phase 1 clinical studies in healthy and elderly volunteers, R4996 (also known as MEM 63908) was generally safe and well tolerated, showed linear, dose-dependent pharmacokinetics with a half-life suitable for once-daily oral dosing, and achieved plasma exposures above those associated with cognitive benefit in preclinical models.[1][4] By partially activating alpha-7 nicotinic acetylcholine receptors, the compound was intended to enhance cognitive function and memory in central nervous system disorders characterized by cognitive impairment.[4][7]
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