Tucci S A, Halford J C G, Harrold J A, Kirkham T C
University of Liverpool, Eleanor Rathbone Building, Bedford Street South, Liverpool L69 7ZA, UK.
Curr Med Chem. 2006;13(22):2669-80. doi: 10.2174/092986706778201512.
Rimonabant (SR141716, Acomplia) has been described as an antagonist/inverse agonist at the cannabinoid receptor type 1 (CB1). It has been widely used as a tool to evaluate the mechanisms by which cannabinoid agonists produce their pharmacological effects and to elucidate the respective physiological or pathophysiological roles of the CB1 receptor. It has become increasingly clear that rimonabant can exert its own intrinsic actions. These may be viewed as evidence of either the inverse agonist nature of rimonabant or of tonic activity of the endocannabinoid system. To date, data obtained from clinical trials (RIO North America, RIO Europe and RIO Lipid) indicate that rimonabant may have clinical benefits in relation to its anti-obesity properties and as a novel candidate for the treatment of metabolic and cardiovascular disorders associated with overweight and obesity. Other clinical trials, such as the STRATUS study, have also shown that rimonabant may be effective in smoking cessation, and that the drug has a reasonable safety profile. Recently, it has been shown that rimonabant prevents indomethacin-induced intestinal injury by decreasing the levels of pro-inflammatory cytokine tumour necrosis factor alpha (TNFalpha), thus indicating that CB1 receptor antagonists might exhibit potential anti-inflammatory activity in acute and chronic diseases.
利莫那班（SR141716，Acomplia）被描述为1型大麻素受体（CB1）的拮抗剂/反向激动剂。它已被广泛用作评估大麻素激动剂产生药理作用的机制以及阐明CB1受体各自的生理或病理生理作用的工具。越来越清楚的是，利莫那班可以发挥其自身的内在作用。这些作用可被视为利莫那班反向激动剂性质或内源性大麻素系统紧张性活动的证据。迄今为止，从临床试验（北美RIO、欧洲RIO和RIO脂质研究）获得的数据表明，利莫那班在抗肥胖特性方面以及作为治疗与超重和肥胖相关的代谢和心血管疾病的新型候选药物可能具有临床益处。其他临床试验，如STRATUS研究，也表明利莫那班在戒烟方面可能有效，并且该药物具有合理的安全性。最近，研究表明利莫那班通过降低促炎细胞因子肿瘤坏死因子α（TNFα）的水平来预防吲哚美辛诱导的肠道损伤，因此表明CB1受体拮抗剂在急性和慢性疾病中可能具有潜在的抗炎活性。
