New tetrazole-based selective anandamide uptake inhibitors

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• 作者：Giorgio Ortar ; Aniello Schiano Moriello ; Maria Grazia Cascio ; Luciano De Petrocellis ; Alessia Ligresti ; Enrico Morera ; Marianna Nalli ; Vincenzo Di Marzo
• 关键词：Endocannabinoids ; Anandamide uptake ; Anandamide uptake inhibitors ; Tetrazoles
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 出版时间：1 May 2008
• 年：2008
• 卷：18
• 期：9
• 页码：2820-2824
• 全文大小：132 K

文摘

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 (IC₅₀ = 2.3–5.1 μM) and selectively over other proteins involved in endocannabinoid action and metabolism.