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[CB1受体抑制与葡萄糖代谢:利莫那班在2型糖尿病中的作用]

[CB1 receptor inhibition and glucose metabolism: role of rimonabant in type 2 diabetes].

作者信息

Scheen André J, Paquot Nicolas, Van Gaal Luc F

机构信息

Service de diabétologie, nutrition et maladies métaboliques, CHU Sart Tilman, 4000 Liège, Belgique.

出版信息

Rev Med Suisse. 2008 Aug 27;4(168):1812-7.

Abstract

Endocannabinoid system is overactivated in individuals with abdominal obesity. CBI receptors, first individualized in the brain, are also expressed in the adipocyte, the skeletal muscle, the liver, the gut, and the pancreas. Their blockade improves glucose tolerance and lipid profile, thanks increased insulin sensitivity and adiponectin levels. Rimonabant, a selective antagonist of CBI receptors, improves glucose control in patients with type 2 diabetes, treated with diet alone, metformin, sulfonylurea or insulin, while it also reduces body weight and other risk factors. Ongoing studies aim at further demonstrating the potential of rimonabant in the management of type 2 diabetes, in the prevention of type 2 diabetes and in the protection against cardiovascular complications in (diabetic) patients with abdominal obesity.

摘要

内源性大麻素系统在腹部肥胖个体中过度激活。大麻素受体1(CBI)最初在大脑中被鉴定出来,也在脂肪细胞、骨骼肌、肝脏、肠道和胰腺中表达。阻断这些受体可改善葡萄糖耐量和血脂状况,这得益于胰岛素敏感性和脂联素水平的提高。利莫那班是一种CBI受体的选择性拮抗剂,在仅通过饮食、二甲双胍、磺脲类药物或胰岛素治疗的2型糖尿病患者中,它可改善血糖控制,同时还能减轻体重并降低其他风险因素。正在进行的研究旨在进一步证明利莫那班在2型糖尿病管理、2型糖尿病预防以及预防腹部肥胖(糖尿病)患者心血管并发症方面的潜力。

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