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S20928 is a naphthalenic small molecule that acts as a non-selective antagonist of melatonin receptors, specifically targeting the MT1 (Mel1a) and MT2 (Mel1b) subtypes. Developed by Servier, it is primarily utilized as a pharmacological research tool to investigate the physiological and pathological roles of melatonin signaling. In preclinical studies, S20928 has been shown to reverse melatonin-mediated effects, including the suppression of tumor growth, inhibition of linoleic acid uptake, and modulation of aerobic glycolysis (the Warburg effect) in various cancer models such as leiomyosarcoma and hepatoma. It also blocks melatonin's influence on vasoconstriction in vascular tissues and its regulatory effects on glucose metabolism and circadian firing rates in the suprachiasmatic nucleus.
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