SR 57746A – (90494-79-4)

Xaliproden, also known as SR57746A, is a potent and selective 5-HT1A receptor agonist with additional properties as a dopamine D2 receptor antagonist. This compound exhibits high affinity for 5-HT1A binding sites in the rat hippocampus and moderate affinity for dopamine D2 receptors. Xaliproden demonstrates anti-depressant and anti-anxiety effects, suggesting potential therapeutic applications in neurodegenerative diseases.

Initially developed by Sanofi, Xaliproden underwent extensive clinical trials for the treatment of Alzheimer’s disease and amyotrophic lateral sclerosis (ALS). In Alzheimer’s disease, two Phase 3 trials involving over 2,700 patients showed no significant improvement in cognitive function as measured by the ADAS-cog or CDR scales, although some studies indicated a reduction in hippocampal atrophy. For ALS, two Phase 3 trials with a combined total of over 2,000 patients also failed to demonstrate a statistically significant treatment benefit.

Despite these setbacks, Xaliproden remains under investigation for its potential in treating chemotherapy-induced peripheral neuropathy due to its neuroprotective properties. The drug’s mechanism of action involves the activation of MAP kinase pathways, which may contribute to its neuroprotective effects.

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Sources:

https://en.wikipedia.org/wiki/Xaliproden
https://pubchem.ncbi.nlm.nih.gov/compound/128918
https://www.medchemexpress.com/xaliproden-hydrochloride.html
https://www.medkoo.com/products/5966
https://www.alzforum.org/therapeutics/xaliproden
https://www.sciencedirect.com/science/article/abs/pii/030645229390429J