PF-04995274 is a potent partial agonist of serotonin 5HT4 receptor with Ki = 0.15?- 0.46 nM for 5-HT4 isoforms a, b, d and e. 5-HT4 agonists modulate cholinergic function are being studied as possible treatment for cognitive disorders associated with Alzheimer′s Disease. PF-04995274 is brain penetrant and was shown to increase brain acetylcholine levels and reversed scopolamine-induced learning deficits in the rat Morris water maze test.
PF-04995274 favors the production of cyclic adenosine monophosphate (cAMP).
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