Cannabinoid receptor type-1: breaking the dogmas.
Cannabinoid receptor type-1: breaking the dogmas.
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DOI：
10.12688/f1000research.8245.1
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发表时间：
2016-01-01
期刊：
影响因子：
--
通讯作者：
Marsicano, Giovanni
中科院分区：
文献类型：
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作者：
Busquets Garcia, Arnau;Soria-Gomez, Edgar;Marsicano, Giovanni
内源性大麻素系统（ECS）在大脑中大量表达。该系统调节众多生理功能，由大麻素受体、其内源性配体（内源性大麻素）以及参与内源性大麻素代谢的酶组成。在这篇综述中，我们强调大麻素信号传导的新进展，重点关注ECS的一个关键成分——1型大麻素受体（CB1）。近年来，新的成像和分子工具的发展表明，该受体可分布在许多细胞类型（例如神经元或神经胶质细胞）以及细胞内区室（例如线粒体）中。有趣的是，根据其特定定位（例如谷氨酸能或γ -氨基丁酸能神经元），CB1受体以不同方式介导细胞和分子效应。此外，该受体在周围组织中表达，在那里它可以调节外周 - 大脑的连接。最后，对CB1受体结构的更好理解促使研究人员提出有趣的新型变构调节剂。因此，CB1受体领域的进展和新方向将为利用其有趣的治疗特性提供新的见解和更好的方法。
The endocannabinoid system (ECS) is abundantly expressed in the brain. This system regulates a plethora of physiological functions and is composed of cannabinoid receptors, their endogenous ligands (endocannabinoids), and the enzymes involved in the metabolism of endocannabinoids. In this review, we highlight the new advances in cannabinoid signaling, focusing on a key component of the ECS, the type-1 cannabinoid receptor (CB 1). In recent years, the development of new imaging and molecular tools has demonstrated that this receptor can be distributed in many cell types (e.g., neuronal or glial cells) and intracellular compartments (e.g., mitochondria). Interestingly, cellular and molecular effects are differentially mediated by CB 1 receptors according to their specific localization (e.g., glutamatergic or GABAergic neurons). Moreover, this receptor is expressed in the periphery, where it can modulate periphery-brain connections. Finally, the better understanding of the CB 1 receptor structure led researchers to propose interesting and new allosteric modulators. Thus, the advances and the new directions of the CB 1 receptor field will provide new insights and better approaches to profit from its interesting therapeutic profile.