内源性大麻素系统:从受体到治疗

Bába László-István, Kolcsár Melinda, Hack Beatrix, Gáll Zsolt, K. Zoltán
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摘要

摘要内源性大麻素系统(endocannabinoid system, ECS)自被发现以来就备受关注。近三十年来的研究进展表明,ECS调节能量代谢的机制多种多样。这些机制可以是中枢机制(调节食欲和卡路里消耗),也可以是外围机制(脂肪细胞特异性和其他)。目前的综述首先强调了导致发现ECS的一些最重要的观察结果,然后详细介绍了这些介质的合成和运输,受体类型和所涉及的第二信使系统。下一部分将专门介绍该系统调节能量代谢的机制。最后,对已进入临床阶段的药物以及未来药物开发的主要靶点和策略进行了综述。
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The endocannabinoid system: from the receptors to therapy
Abstract The endocannabinoid system (ECS) received a lot of attention ever since its discovery. Advancements of the last three decades have shown that there are numerous mechanisms by which the ECS regulates the energy metabolism. These can either be central (regulating appetite and calorie expenditure) or peripheral (adipocyte-specific and other) mechanisms. The current review highlights some of the most important observations leading to the discovery of the ECS first, followed by a part detailing the synthesis and transport of these mediators, the receptor types and second messenger systems involved. The next part is dedicated to the mechanisms by which this system regulates the energy metabolism. Lastly, the drugs that reached the clinical phase and the main targets and strategies for future drug development will be reviewed.
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