Cayman AM251

AM251 is a cannabinoid 1 (CB₁) receptor 1 antagonist.¹ It binds to CB₁ receptors in rat forebrain membrane preparations (K_i = 7.5 nM) and is selective over CB₂ receptors in mouse spleen preparations (K_i = 2,290 nM) in radioligand binding assays. AM251 inhibits GTPγS binding induced by the CB receptor agonist CP 55,940 in HEK293 cells expressing human CB₁ receptors (EC₅₀ = 8 nM).² AM251 (10 mg/kg) decreases immobility time in the forced swim test in wild-type but not CB₁ receptor-deficient mice.³ It reduces fasting-induced food intake and body weight gain in mice when administered at a dose of 30 mg/kg. AM251 also induces GTPγS binding in HEK293 cells expressing the orphan receptor GPR55 (EC₅₀ = 39 nM) and potentiates GABA-induced GABA_A receptor currents (EC₅₀ = 0.4 µM).^2,4 It prevents TGF-β1-induced epithelial-to-mesenchymal transition (EMT), inhibits SMAD2/3 and p38 MAPK activation, and reduces the expression of EMT-related transcription factors in HK-2 renal tubule epithelial cells.⁵ AM251 induces cell cycle arrest at the g₂/M phase and apoptosis in A375 human melanoma cells.⁶

WARNING This product is not for human or veterinary use.