Evidence suggests 5-HT4 receptor agonists act as pro-cognitive agents and may provide therapeutic relief for cognitive impairments associated with Alzheimer's disease (AD).  A hallmark of AD is a reduction in acetylcholine levels (ACh) resulting from a loss of cholinergic neurons which contributes to cognitive impairment.  5-HT4 agonists reportedly increase brain ACh levels and reverse memory deficits induced by cholinergic antagonists in behavioral studies.  In addition, 5-HT4 receptor agonism is reported to increases hippocampal theta activity; a response that is modulated by ACh and linked to several cognitive, memory and attentional processes.  Herein, we report the discovery and characterization of the 5-HT4 receptor agonist PF-04995274.

5HT4 partial agonists to improve cognitive dysfunction in learning and memory disorders: Discovery of PF-4995274

243rd National Meeting (2012)

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