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PRX-03140 is an orally bioavailable small molecule that acts as a selective partial agonist of the 5-Hydroxytryptamine receptor 4 (5-HT4) and also binds to Sigma-1 and Sigma-2 receptors. It was developed by EPIX Pharmaceuticals for the treatment of Alzheimer's disease. The drug demonstrates high selectivity for the human 5‑HT4 receptor (Ki = 14.3 nM), with minimal affinity for other serotonin receptors or unrelated targets. In preclinical studies and early clinical trials, PRX‑03140 showed potential to improve cognitive function by increasing acetylcholine release in the brain and stimulating non‑amyloidogenic processing of amyloid precursor protein (APP), which may slow Alzheimer’s disease progression. The compound reached Phase II clinical trials but development appears to be inactive[1][2][5][6][7].
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