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GSK-1521498 is an investigational small molecule drug developed by GSK (formerly GlaxoSmithKline) as a selective inverse agonist of the mu-opioid receptor. It is orally administered and has been studied primarily for the treatment of obesity, binge eating, and alcohol use disorder. The drug acts by inhibiting the effects of endogenous opioids (such as endorphins), which are involved in regulating hedonic responses to food and addictive behaviors. Preclinical and clinical studies indicate that it reduces hedonic responses to palatable foods and caloric intake, particularly high-fat foods, with dose-dependent pharmacodynamic effects. It is >10-fold selective for the human mu-opioid receptor compared to kappa or delta opioid receptors[1][2][3][4][5][9].
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