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在人和大鼠的脑及外周组织中分离并测定内源性大麻素受体激动剂花生四烯乙醇胺。

Isolation and measurement of the endogenous cannabinoid receptor agonist, anandamide, in brain and peripheral tissues of human and rat.

作者信息

Felder C C, Nielsen A, Briley E M, Palkovits M, Priller J, Axelrod J, Nguyen D N, Richardson J M, Riggin R M, Koppel G A, Paul S M, Becker G W

机构信息

Laboratory of Cell Biology, National Institute of Mental Health, Bethesda, MD 20892-4090, USA.

出版信息

FEBS Lett. 1996 Sep 16;393(2-3):231-5. doi: 10.1016/0014-5793(96)00891-5.

DOI:10.1016/0014-5793(96)00891-5
PMID:8814296
Abstract

Anandamide (arachidonylethanolamide) is a novel lipid neurotransmitter first isolated from porcine brain which has been shown to be a functional agonist for the cannabinoid CB1 and CB2 receptors. Anandamide has never been isolated from human brain or peripheral tissues and its role in human physiology has not been examined. Anandamide was measured by LC/MS/MS and was found in human and rat hippocampus (and human parahippocampal cortex), striatum, and cerebellum, brain areas known to express high levels of CB1 cannabinoid receptors. Significant levels of anandamide were also found in the thalamus which expresses low levels of CB1 receptors. Anandamide was also found in human and rat spleen which expresses high levels of the CB2 cannabinoid receptor. Small amounts of anandamide were also detected in human heart and rat skin. Only trace quantities were detected in pooled human serum, plasma, and CSF. The distribution of anandamide in human brain and spleen supports its potential role as an endogenous agonist in central and peripheral tissues. The low levels found in serum, plasma, and CSF suggest that it is metabolized in tissues where it is synthesized, and that its action is probably not hormonal in nature.

摘要

花生四烯酸乙醇胺(N-花生四烯酸乙醇胺)是一种新型脂质神经递质,最初从猪脑中分离出来,已被证明是大麻素CB1和CB2受体的功能性激动剂。花生四烯酸乙醇胺从未从人脑中或外周组织中分离出来,其在人体生理学中的作用也未得到研究。通过液相色谱/串联质谱法对花生四烯酸乙醇胺进行测定,结果在人和大鼠的海马体(以及人的海马旁皮质)、纹状体和小脑中发现了它,这些脑区已知表达高水平的CB1大麻素受体。在表达低水平CB1受体的丘脑中也发现了显著水平的花生四烯酸乙醇胺。在表达高水平CB2大麻素受体的人和大鼠脾脏中也发现了花生四烯酸乙醇胺。在人的心脏和大鼠的皮肤中也检测到少量的花生四烯酸乙醇胺。在人血清、血浆和脑脊液的混合样本中仅检测到痕量。花生四烯酸乙醇胺在人脑中的分布及其在脾脏中的存在,支持了它作为中枢和外周组织中内源性激动剂的潜在作用。在血清、血浆和脑脊液中发现的低水平表明,它在合成部位的组织中被代谢,其作用可能本质上并非激素作用。

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