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内源性大麻素系统——心脏代谢风险的新靶点。

Endocannabinoid system--a novel target for cardiometabolic risk.

作者信息

Joshi Shashank R

机构信息

Lilavati Hospital, Mumbai.

出版信息

J Assoc Physicians India. 2007 Jun;55:439-44.

Abstract

The endocannabinoid system (EC) plays a significant role in appetite drive and associated behaviours. Therefore attenuation of the activity of the EC system would have therapeutic benefit in treating disorders that might have a component of excess appetite drive or over-activity of the endocannabinoid system, such as obesity, ethanol and other drug abuse, and a variety of central nervous system and other disorders. Antagonists of cannabinoid receptors have been designed through rational drug discovery essential to exploit these novel targets for potential in obesity, metabolism, addiction, pain and neurologic disorders. Rimonabant is the only compound in this group which along this pathway is now approved as a selective CB (1) (cannabinoid receptor subtype 1) antagonist, or inverse agonist, in the European Union and India and under regulatory review in the United States for the treatment of obesity and associated cardiometabolic risk.

摘要

内源性大麻素系统(EC)在食欲驱动及相关行为中发挥着重要作用。因此,减弱EC系统的活性对于治疗那些可能存在食欲驱动过度或内源性大麻素系统活性过强的疾病具有治疗益处,这些疾病包括肥胖症、乙醇及其他药物滥用,以及多种中枢神经系统疾病和其他病症。通过合理的药物研发设计出了大麻素受体拮抗剂,这对于开发这些新靶点在肥胖、代谢、成瘾、疼痛和神经系统疾病方面的潜力至关重要。利莫那班是该类化合物中唯一一种沿着此途径现已在欧盟和印度被批准作为选择性CB(1)(大麻素受体亚型1)拮抗剂或反向激动剂,且在美国正处于监管审查阶段用于治疗肥胖症及相关心脏代谢风险的药物。

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