Ducobu J
Service de Médecine, C.H.U. Tivoli, La Louvière, U.L.B.
J Pharm Belg. 2005;60(3):84-8.
The endocannabinoid system modulates many physiological functions by acting on receptors CB1 and CB2. The endocannabinoids are produced only when and where they are needed. They act locally and are immediately metabolised after their action. Overactivation of the endocannabinoid system is observed in obesity, with stimulation of the appetite in the hypothalamus and fat accumulation in the adipocytes with increase of insulin resistance and decrease of adiponectin. Nicotine use overactivates also the endocannabinoid system. CB1 blockade by a specific inhibitor (rimonabant) decreases food intake and weight in animal studies and increases adiponectin and insulin sensitivity. Moreover, rimonabant decreases tobacco dependence. Clinical studies with rimonabant are encouraging.
内源性大麻素系统通过作用于CB1和CB2受体来调节多种生理功能。内源性大麻素仅在需要的时间和地点产生。它们在局部起作用,作用后立即被代谢。在肥胖症中观察到内源性大麻素系统过度激活,伴有下丘脑食欲刺激以及脂肪细胞中脂肪堆积,同时胰岛素抵抗增加和脂联素减少。使用尼古丁也会使内源性大麻素系统过度激活。在动物研究中,用一种特异性抑制剂(利莫那班)阻断CB1可减少食物摄入量和体重,并增加脂联素和胰岛素敏感性。此外,利莫那班可降低烟草依赖性。有关利莫那班的临床研究令人鼓舞。