Description
AM251 binds to cannabinoid (CB) receptors with Ki values of 7.5 and 2,290 nM for CB1 and CB2 from rat forebrain and mouse spleen, respectively.1 It acts as an antagonist at CB1 and an inverse agonist at CB2 receptors.1,2 It also acts as an agonist at GPR55 (EC50 = 39 nM) and potentiates GABAA receptor currents (EC50 = 0.4 µM).3,4 AM251 prevents TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in HK-2 renal tubule epithelial cells through mechanisms independent of CB receptors or GPR55.5 It inhibits SMAD2/3 and p38 MAPK activation and the expression of EMT-related transcription factors. It has additional anticancer activities, including halting the cell cycle at the G2/M phase and inducing apoptosis in A375 human melanoma cells.6 In mice, AM251 reduces antidepressant-like behavior in the tail suspension and forced swim tests and decreases hyperphagia induced by fasting.7WARNING This product is not for human or veterinary use.
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