Cayman Rimonabant

Rimonabant is a cannabinoid 1 (CB₁) receptor antagonist (K_i = 5.6 nM). It is selective for CB₁ over CB₂ receptors (K_i = >1,000 nM), as well as a panel of 37 other receptors and channels (IC₅₀s = >1,000 nM). Rimonabant (10 µM) inhibits phytohemagglutinin-induced proliferation of isolated human peripheral blood mononuclear cells (PBMCs). Intraperitoneal administration of rimonabant prevents decreases in body temperature and increases in tail-flick latency induced by the CB₁ and CB₂ receptor agonist (+)-WIN 55,212-2 (Item No. ) in mice (ED₅₀s = 0.28 and 1.62 mg/kg, respectively) and oral administration reduces body weight in a mouse model of diet-induced obesity when administered at a dose of 10 mg/kg in the drinking water.^, Rimonabant (10 mg/kg) decreases the percentage of time spent in the open arms of the elevated plus maze in mice, indicating anxiety-like activity. Formulations containing rimonabant have previously been used in the treatment of obesity.

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