Rimonabant

Rimonabant is a cannabinoid 1 (CB₁) receptor antagonist (K_i = 5.6 nM).¹ 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).² 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. 10009023) 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.^1,3 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.⁴ Formulations containing rimonabant have previously been used in the treatment of obesity.

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1. Rinaldi-Carmona, M., Barth, F., Héaulme, M., et al. SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett. 350(2-3), 240-244 (1994).

2. Malfitano, A.M., Laezza, C., Pisanti, S., et al. Rimonabant (SR141716) exerts anti-proliferative and immunomodulatory effects in human peripheral blood mononuclear cells. Br. J. Pharmacol. 153(5), 1003-1010 (2009).

3. Lee, S.H., Seo, H.J., Lee, S.H., et al. Biarylpyrazolyl oxadiazole as potent, selective, orally bioavailable cannabinoid-1 receptor antagonists for the treatment of obesity. J. med. Chem. 51(22), 7216-7233 (2008).

4. Bellocchio, L., Soria-Gómez, E., Quarta, C., et al. Activation of the sympathetic nervous system mediates hypophagic and anxiety-like effects of CB₁ receptor blockade. Proc. Natl. Acad. Sci. USA 110(12), 4786-4791 (2013).

Myers, M.N., Abou-Rjeileh, U., Chirivi, M., et al. Cannabinoid-1 receptor activation modulates lipid mobilization and adipogenesis in the adipose tissue of dairy cows. J. Dairy Sci. 106(5), 3650-3661 (2023).

McDougle, D.R., Watson, J.E., Abdeen, A.A., et al. Anti-inflammatory ω-3 endocannabinoid epoxides. Proc. Natl. Acad. Sci. USA 114(30), E6034-E6043 (2017).