Synthesis and Pharmacological Activity of a Potent Inhibitor of the Biosynthesis of the Endocannabinoid 2-Arachidonoylglycerol

被引：35

作者：

Bisogno, Tiziana ^{[1
]}

Burston, James J. ^{[2
]}

Rai, Ravi ^{[3
]}

Allara, Marco ^{[1
]}

Saha, Bijali ^{[3
]}

Mahadevan, Anu ^{[3
]}

Razdan, Raj K. ^{[3
]}

Wiley, Jenny L. ^{[2
]}

Di Marzo, Vincenzo ^{[1
]}

机构：

[1] CNR, Inst Biomol Chem, Endocannabinoid Res Grp, Pozzuali, NA, Italy

[2] Virginia Commonwealth Univ, Dept Pharmacol & Toxicol, Richmond, VA 23298 USA

[3] Organix Inc, Woburn, MA 01801 USA

来源：

CHEMMEDCHEM | 2009年 / 4卷 / 06期

基金：

美国国家卫生研究院;

关键词：

biosynthesis; CB1; DAGL; endocannabinoids; cannabinoids; receptors; FOOD-INTAKE; SYSTEM;

D O I：

10.1002/cmdc.200800442

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

(Chemical Equation Presented) Biosynthesis Inhibition: O-5596, a new inhibitor of the biosynthesis of the endocannabinoid, 2-arachidonoylglycerol, was synthesized and found to be potent (IC50=100 nm) and selective versus other proteins and enzymes of the endocannabinoid system in vitro and active in vivo at reducing food intake in mice. © 2009 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：946 / 950

页数：5

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