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首页> 外文期刊>Expert opinion on therapeutic targets >Muscarinic acetylcholine receptors as therapeutic targets for obesity.
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Muscarinic acetylcholine receptors as therapeutic targets for obesity.

机译：毒蕈碱型乙酰胆碱受体作为肥胖症的治疗靶标。

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BACKGROUND: There are five types of muscarinic acetylcholine receptors (mAChRs), M(1) - M(5), which regulate several central and peripheral functions. Transgenic mice deficient in these receptors have been generated. OBJECTIVE: To understand some processes in which these receptors are involved, mainly targeting obesity, which seems to be mediated by M(3) in the hypothalamus. METHODS: The absence of M(3) has beneficial effects, which protect mice against some forms of obesity and ameliorate glucose and energy homeostasis. These findings suggest some relevance of muscarinic M(3) antagonists to the treatment of obesity, and also studies with new classes of M(3)-receptor selective antagonists, to identify active/selective molecules, able to reach the CNS, which might have fewer side-effects compared with available muscarinic drugs. RESULTS/CONCLUSION: M(3) antagonists might have application to the design of antiobesity agents. However, this research is in its preliminary phases, and the lack of specific antagonists or agonists for M(3) receptors in CNS, make it impossible to validate this antiobesity target at present.
机译：背景：毒蕈碱乙酰胆碱受体（mAChRs）有五种类型，M（1）-M（5），它们调节几种中枢和外周功能。已经产生了缺乏这些受体的转基因小鼠。目的：了解一些涉及这些受体的过程，这些过程主要针对肥胖，这似乎是由下丘脑中的M（3）介导的。方法：缺乏M（3）具有有益的作用，可以保护小鼠免受某些形式的肥胖症并改善葡萄糖和能量稳态。这些发现表明毒蕈碱型M（3）拮抗剂与肥胖症的治疗具有一定的相关性，并且还研究了新型M（3）-受体选择性拮抗剂，以鉴定能够到达中枢神经系统的活性/选择性分子，这可能与与毒蕈碱类药物相比，副作用更少。结果/结论：M（3）拮抗剂可能已应用于减肥药的设计。但是，这项研究尚处于初步阶段，并且中枢神经系统中缺少M（3）受体的特异性拮抗剂或激动剂，因此目前尚无法验证该抗肥胖目标。

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