Vogel Z, Barg J, Levy R, Saya D, Heldman E, Mechoulam R
Department of Neurobiology, Weizmann Institute of Science, Rehovot, Israel.
J Neurochem. 1993 Jul;61(1):352-5. doi: 10.1111/j.1471-4159.1993.tb03576.x.
A putative endogenous cannabinoid ligand, arachidonylethanolamide (termed "anandamide"), was isolated recently from porcine brain. Here we demonstrate that this compound is a specific cannabinoid agonist and exerts its action directly via the cannabinoid receptors. Anandamide specifically binds to membranes from cells transiently (COS) or stably (Chinese hamster ovary) transfected with an expression plasmid carrying the cannabinoid receptor DNA but not to membranes from control nontransfected cells. Moreover, anandamide inhibited the forskolin-stimulated adenylate cyclase in the transfected cells and in cells that naturally express cannabinoid receptors (N18TG2 neuroblastoma) but not in control nontransfected cells. As with exogenous cannabinoids, the inhibition by anandamide of the forskolin-stimulated adenylate cyclase was blocked by treatment with pertussis toxin. These data indicate that anandamide is an endogenous agonist that may serve as a genuine neurotransmitter for the cannabinoid receptor.
一种假定的内源性大麻素配体——花生四烯酸乙醇胺（称为“花生四烯酸酰胺”），最近从猪脑中分离出来。在此我们证明，该化合物是一种特异性大麻素激动剂，并通过大麻素受体直接发挥作用。花生四烯酸酰胺特异性结合于用携带大麻素受体DNA的表达质粒瞬时（COS）或稳定（中国仓鼠卵巢细胞）转染的细胞的膜，但不结合于对照未转染细胞的膜。此外，花生四烯酸酰胺抑制转染细胞以及天然表达大麻素受体的细胞（N18TG2神经母细胞瘤细胞）中福斯高林刺激的腺苷酸环化酶活性，但不抑制对照未转染细胞中的该活性。与外源性大麻素一样，花生四烯酸酰胺对福斯高林刺激的腺苷酸环化酶的抑制作用可被百日咳毒素处理所阻断。这些数据表明，花生四烯酸酰胺是一种内源性激动剂，可能作为大麻素受体的真正神经递质。
