PF-04995274 favors the production of cyclic adenosine monophosphate (cAMP).[1]
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.
Journal of medicinal chemistry, 55(21), 9240-9254 (2012-09-15)
The cognitive impairments observed in Alzheimer's disease (AD) are in part a consequence of reduced acetylcholine (ACh) levels resulting from a loss of cholinergic neurons. Preclinically, serotonin 4 receptor (5-HT(4)) agonists are reported to modulate cholinergic function and therefore may
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