Di Marzo V, Szallasi A
Endocannabinoid Research Group, Institute of Biomolecular Chemistry, C.N.R., Pozzuoli (NA), Italy.
Br J Pharmacol. 2008 Jul;154(5):915-7. doi: 10.1038/bjp.2008.170. Epub 2008 May 5.
The synthetic cannabinoid CB1 receptor antagonist rimonabant (sold in the United Kingdom under the brand name Acomplia) was reported to improve the profile of cardiovascular risk factors in obese patients with the metabolic syndrome, a cluster of metabolic disorders that often precedes the onset of type II diabetes. Rimonabant is shown in the current issue of British Journal of Pharmacology to attenuate weight gain in Zucker rats, an experimental model of insulin resistance. Neutrophil and monocyte counts were lowered by rimonabant administration. Both platelet activation (by ADP) and aggregation (in response to thrombin) were inhibited. Circulating pro-inflammatory cytokine levels (monocyte chemotactic protein 1, MCP1 and Regulated upon Activation, Normal T-cell Expressed and Secreted, RANTES) were also reduced. Furthermore, fibrinogen levels returned to normal. These favourable anti-inflammatory and anti-thrombotic actions imply for rimonabant a peripheral, direct action on some cardiovascular risk factors.
据报道，合成大麻素CB1受体拮抗剂利莫那班（在英国以Acomplia品牌销售）可改善患有代谢综合征的肥胖患者的心血管危险因素状况，代谢综合征是一组常常先于II型糖尿病发作的代谢紊乱症候群。在本期《英国药理学期刊》中显示，利莫那班可减轻胰岛素抵抗实验模型——Zucker大鼠的体重增加。给予利莫那班可降低中性粒细胞和单核细胞计数。利莫那班抑制了（由二磷酸腺苷引起的）血小板活化以及（对凝血酶的反应）血小板聚集。循环促炎细胞因子水平（单核细胞趋化蛋白1，MCP1以及活化调节正常T细胞表达和分泌因子，RANTES）也有所降低。此外，纤维蛋白原水平恢复正常。这些有利的抗炎和抗血栓作用表明利莫那班对某些心血管危险因素具有外周直接作用。
