MOLECULAR CHARACTERIZATION OF A PERIPHERAL RECEPTOR FOR CANNABINOIDS
MOLECULAR CHARACTERIZATION OF A PERIPHERAL RECEPTOR FOR CANNABINOIDS
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DOI：
10.1038/365061a0
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发表时间：
1993-09-02
期刊：
影响因子：
64.8
通讯作者：
ABUSHAAR, M
中科院分区：
文献类型：
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作者：
MUNRO, S;THOMAS, KL;ABUSHAAR, M
大麻的主要活性成分Delta9-四氢大麻酚(Delta9-THC)被用作精神活性物质已有数千年的历史。大麻和Delta9-THC还发挥着广泛的其他作用，包括止痛、抗炎、免疫抑制、抗惊厥、减轻青光眼的眼压和减少呕吐。然而，大麻素的临床应用一直受到其精神活性作用的限制，这导致了人们对其作用的生化基础的兴趣。进展最初源于Delta9-THC4，5的有效衍生物的合成，以及最近编码大麻素的G蛋白偶联受体6的基因的克隆。这种受体在大脑中表达，但在外周不表达，除了在睾丸中的低水平表达。有人认为大麻素的非精神活性作用是通过中枢或通过与其他非受体蛋白1、7、8的直接相互作用来实现的。在这里，我们报道了一种大麻素受体的克隆，该受体不在大脑中表达，而是在脾边缘区的巨噬细胞中表达。
THE major active ingredient of marijuana, DELTA9-tetrahydrocannabinol (DELTA9-THC), has been used as a psychoactive agent for thousands of years. Marijuana, and DELTA9-THC, also exert a wide range of other effects including analgesia, anti-inflammation, immunosuppression, anticonvulsion, alleviation of intraocular pressure in glaucoma, and attenuation of vomiting1. The clinical application of cannabinoids has, however, been limited by their psychoactive effects, and this has led to interest in the biochemical bases of their action. Progress stemmed initially from the synthesis of potent derivatives of DELTA9-THC4,5, and more recently from the cloning of a gene encoding a G-protein-coupled receptor for cannabinoids6. This receptor is expressed in the brain but not in the periphery, except for a low level in testes. It has been proposed that the non-psychoactive effects of cannabinoids are either mediated centrally or through direct interaction with other, non-receptor proteins1,7,8. Here we report the cloning of a receptor for cannabinoids that is not expressed in the brain but rather in macrophages in the marginal zone of spleen.