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新型内源性大麻素系统的天然和合成配体。

Novel natural and synthetic ligands of the endocannabinoid system.

机构信息

Institute for Drug Research, Hebrew University, Jerusalem, Israel.

出版信息

Curr Med Chem. 2010;17(14):1341-59. doi: 10.2174/092986710790980096.

Abstract

In this review we describe recent advances in the chemistry of novel CB(1)/CB(2) agonists, CB(1) antagonists, selective CB(2) agonists, fatty acid amide hydrolase inibitors, monoglyceride (MGL) and diglyceride (DAGL) inhibitors and cannabinoid-type agonists and antagonists of non CB(1)/CB(2) receptors. In view of recent interest in the activities of fatty acid amides of amino acids (N-acyl amino acids) a list of this type of compounds was compiled and is presented as a Table. We conclude that further synthetic work based on both the plant cannabinoids and on the endocannabinoids may lead to novel therapeutics and that the identification and the elucidation of the biological profile of the myriad of endogenous N-acyl amino acids and related compounds may enhance the already wide spectrum of lipidomics.

摘要

在这篇综述中,我们描述了新型 CB(1)/CB(2) 激动剂、CB(1)拮抗剂、选择性 CB(2) 激动剂、脂肪酸酰胺水解酶抑制剂、单甘油酯 (MGL) 和二甘油酯 (DAGL) 抑制剂以及非 CB(1)/CB(2) 受体的大麻素型激动剂和拮抗剂的化学研究进展。鉴于人们对氨基酸脂肪酸酰胺(N-酰基氨基酸)的活性的近期兴趣,我们编制了此类化合物的列表,并以表格形式呈现。我们得出结论,基于植物大麻素和内源性大麻素的进一步合成工作可能会导致新的治疗方法,而内源性 N-酰基氨基酸和相关化合物的鉴定和阐明可能会扩展脂质组学的广泛范围。

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