Cannabinoid receptors and their endogenous ligands.

Cannabinoid receptors and their endogenous ligands.
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大麻素受体及其内源性配体。

DOI:
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发表时间:
2002
期刊:
Journal of Biochemistry (Tokyo)
影响因子:
--
通讯作者:
K. Waku
K. Waku
中科院分区:
--
文献类型:
--
作者:
T. Sugiura;K. Waku

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Delta9-四氢大麻酚是大麻的主要精神活性成分,已被证明与特定的大麻素受体相互作用,从而在实验动物和人类中引起多种药理反应。 1990年,编码大麻素受体(CB1)的基因被克隆。这促使人们寻找内源配体。 1992年,从猪脑中分离出N-花生四烯酰乙醇胺(anandamide)作为内源性配体,1995年,从大鼠脑和犬肠道中分离出2-花生四烯酰甘油作为另一种内源性配体。 anandamide 和 2-arachidonoylglycerol 均表现出各种大麻模拟活性。然而,结构-活性关系实验的结果表明,2-花生四烯酰甘油,而不是花生四烯酸乙醇胺,是大麻素受体的内在天然配体。 2-花生四烯酰甘油是肌醇磷脂的降解产物,它将大麻素受体的功能与受刺激的组织和细胞中增强的肌醇磷脂周转联系起来。讨论了大麻素受体和 2-花生四烯酰甘油在各种哺乳动物组织(例如神经系统组织)中可能的生理作用。
Delta9-Tetrahydrocannabinol, a major psychoactive component of marijuana, has been shown to interact with specific cannabinoid receptors, thereby eliciting a variety of pharmacological responses in experimental animals and human. In 1990, the gene encoding a cannabinoid receptor (CB1) was cloned. This prompted the search for endogenous ligands. In 1992, N-arachidonoylethanolamine (anandamide) was isolated from pig brain as an endogenous ligand, and in 1995, 2-arachidonoylglycerol was isolated from rat brain and canine gut as another endogenous ligand. Both anandamide and 2-arachidonoylglycerol exhibit various cannabimimetic activities. The results of structure-activity relationship experiments, however, revealed that 2-arachidonoylglycerol, but not anandamide, is the intrinsic natural ligand for the cannabinoid receptor. 2-Arachidonoylglycerol is a degradation product of inositol phospholipids that links the function of cannabinoid receptors with the enhanced inositol phospholipid turnover in stimulated tissues and cells. The possible physiological roles of cannabinoid receptors and 2-arachidonoylglycerol in various mammalian tissues such as those of the nervous system are discussed.
DOI: 10.1016/s0021-9258(18)33114-4
发表时间: 1983-01
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影响因子: --
作者:
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DOI: --
发表时间: 1995
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影响因子: --
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发表时间: 1998-04-01
影响因子: 3.6
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期刊: SCIENCE
影响因子: 56.9
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