新型基于四氮唑的选择性花生四烯酸乙醇胺摄取抑制剂。
New tetrazole-based selective anandamide uptake inhibitors.
作者信息
Ortar Giorgio, Schiano Moriello Aniello, Cascio Maria Grazia, De Petrocellis Luciano, Ligresti Alessia, Morera Enrico, Nalli Marianna, Di Marzo Vincenzo
机构信息
Dipartimento di Studi Farmaceutici, Sapienza Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy.
出版信息
Bioorg Med Chem Lett. 2008 May 1;18(9):2820-4. doi: 10.1016/j.bmcl.2008.04.003. Epub 2008 Apr 4.
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.
已合成了一系列新的1,5 - 和2,5 - 二取代四唑，并作为花生四烯酸乙醇胺细胞摄取抑制剂进行了评估。其中一些化合物以相对较高的效力（IC(50)=2.3 - 5.1微摩尔）抑制摄取过程，并且相对于参与内源性大麻素作用和代谢的其他蛋白质具有选择性。
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