Battista Natalia, Bari Monica, Finazzi-Agrò Alessandro, Maccarrone Mauro
Department of Experimental Medicine and Biochemical Sciences, University of Rome Tor Vergata, Rome, Italy.
Lipids Health Dis. 2002 Sep 3;1:1. doi: 10.1186/1476-511x-1-1.
Anandamide (N-arachidonoylethanolamine, AEA) belongs to an emerging class of endogenous lipids, called "endocannabinoids". A specific AEA membrane transporter (AMT) allows the import of this lipid and its degradation by the intracellular enzyme AEA hydrolase. Here, we show that synaptosomes from human, mouse and rat brain might be an ideal ex vivo system for the study of: i) the accumulation of AEA in brain, and ii) the pharmacological properties of AMT inhibitors. Using this ex vivo system, we demonstrate for the first time that glutamine and glutamate act as non-competitive inhibitors of AEA uptake by human, mouse and rat brain AMT.
花生四烯酸乙醇胺（N-花生四烯酰乙醇胺，AEA）属于一类新出现的内源性脂质，称为“内源性大麻素”。一种特定的AEA膜转运蛋白（AMT）可使这种脂质进入细胞，并由细胞内的AEA水解酶将其降解。在此，我们表明，来自人、小鼠和大鼠大脑的突触体可能是用于研究以下方面的理想离体系统：i）AEA在大脑中的蓄积，以及ii）AMT抑制剂的药理特性。利用这个离体系统，我们首次证明谷氨酰胺和谷氨酸作为人、小鼠和大鼠大脑AMT摄取AEA的非竞争性抑制剂。
