作者:Giorgio Ortar、Aniello Schiano Moriello、Maria Grazia Cascio、Luciano De Petrocellis、Alessia Ligresti、Enrico Morera、Marianna Nalli、Vincenzo Di Marzo
DOI:10.1016/j.bmcl.2008.04.003
日期:2008.5
A new series of 1,5- and 2,5-disubstituted tetrazoles have been synthesized and evaluated as inhibitors of anandamide cellular uptake. Some of them inhibit the uptake process with a relatively high potency (IC(50)=2.3-5.1microM) and selectively over other proteins involved in endocannabinoid action and metabolism.
已经合成了一系列新的1,5-和2,5-二取代的四唑并作为anandamide细胞摄取的抑制剂进行了评估。其中一些以相对较高的效力(IC(50)= 2.3-5.1microM)抑制摄取过程,并选择性地超过参与内源性大麻素作用和代谢的其他蛋白质。