ISOLATION AND STRUCTURE OF A BRAIN CONSTITUENT THAT BINDS TO THE CANNABINOID RECEPTOR
ISOLATION AND STRUCTURE OF A BRAIN CONSTITUENT THAT BINDS TO THE CANNABINOID RECEPTOR
复制标题
DOI：
10.1126/science.1470919
复制
发表时间：
1992-12-18
期刊：
影响因子：
56.9
通讯作者：
MECHOULAM, R
中科院分区：
文献类型：
--
作者：
DEVANE, WA;HANUS, L;MECHOULAM, R
花生四烯酸衍生物花生四烯酸乙醇酰胺，在猪脑中，被确定在大麻素受体的内源性配体的屏幕。该化合物的结构已被命名为“anandamide”，通过质谱和核磁共振光谱确定，并通过合成确认。Anandamide抑制特异性结合的放射性标记的大麻素探针的突触体膜的方式典型的竞争性配体，并产生浓度依赖性抑制电诱发的抽搐反应的小鼠输精管，精神大麻素的特征性效果。这些性质表明，大麻素酰胺可能作为大麻素受体的天然配体发挥作用。
Arachidonylethanolamide, an arachidonic acid derivative in porcine brain, was identified in a screen for endogenous ligands for the cannabinoid receptor. The structure of this compound, which has been named "anandamide," was determined by mass spectrometry and nuclear magnetic resonance spectroscopy and was confirmed by synthesis. Anandamide inhibited the specific binding of a radiolabeled cannabinoid probe to synaptosomal membranes in a manner typical of competitive ligands and produced a concentration-dependent inhibition of the electrically evoked twitch response of the mouse vas deferens, a characteristic effect of psychotropic cannabinoids. These properties suggest that anandamide may function as a natural ligand for the cannabinoid receptor.