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
收藏
页码：946 / 950
页数：5
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