Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors

被引：59

作者：

López-Rodríguez, ML

Viso, A

Ortega-Gutiérrez, S

Lastres-Becker, I

González, S

Fernández-Ruiz, J

Ramos, JA

机构：

[1] Univ Complutense, Fac Ciencias Quim, Dept Quim Organ 1, E-28040 Madrid, Spain

[2] Univ Complutense, Fac Med, Dept Bioquim & Biol Mol 3, E-28040 Madrid, Spain

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2001年 / 44卷 / 26期

关键词：

D O I：

10.1021/jm015545y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In the present work, we have designed and synthesized a series of arachidonic acid derivatives of general structure I which have been characterized as highly potent and selective inhibitors of anandamide transporter (IC50 = 24-0.8 muM, K-i > 1000-5000 nM for CB1 and CB2 cannabinoid receptors and vanilloid VR1 receptor). Among them N-(3-furylmethyl)eicosa-5,8,11,14-tetraenamide deserves special attention as being the most potent endocannabinoid transporter inhibitor (IC50 = 0.8 muM) described to date.

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页码：4505 / 4508

页数：4

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