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URB597 is a potent, selective, and irreversible small-molecule inhibitor of fatty acid amide hydrolase (FAAH), the principal enzyme responsible for intracellular hydrolysis of the endocannabinoid anandamide.[1][4][7] By inhibiting FAAH, URB597 elevates anandamide and related lipid mediator levels in vivo, enhancing endogenous cannabinoid signaling primarily through cannabinoid CB1 and CB2 receptors without directly binding or activating them.[1][4][7] URB597 shows antinociceptive (analgesic), anti-inflammatory, anxiolytic, and potential antineoplastic activity in preclinical models, and its mechanism is pharmacologically distinct from exogenous cannabinoid receptor agonists. It has been explored preclinically for potential use in pain, anxiety, addiction, and cancer.[1][3][6][7]
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