Applying a multitarget rational drug design strategy: the first set of modulators with potent and balanced activity toward dopamine D3 receptor and fatty acid amide hydrolase

被引：25

作者：

De Simone, Alessio ^{[1
]}

Ruda, Gian Filippo ^{[1
]}

Albani, Clara ^{[1
]}

Tarozzo, Glauco ^{[1
]}

Bandiera, Tiziano ^{[1
]}

Piomelli, Daniele ^{[1
,2
]}

Cavalli, Andrea ^{[1
,3
]}

Bottegoni, Giovanni ^{[1
]}

机构：

[1] Ist Italiano Tecnol, Dept Drug Discovery & Dev, I-16163 Genoa, Italy

[2] Univ Calif Irvine, Dept Pharmacol, Irvine, CA 92697 USA

[3] Univ Bologna, Dept Pharm & Biotechnol, I-40126 Bologna, Italy

来源：

CHEMICAL COMMUNICATIONS | 2014年 / 50卷 / 38期

关键词：

NICOTINE ADDICTION; D-3; INHIBITORS; DISCOVERY; LIGANDS; ANTAGONISTS; URB597; FAAH; POLYPHARMACOLOGY; SELECTIVITY;

D O I：

10.1039/c4cc00967c

中图分类号：

O6 [化学];

学科分类号：

070301 [无机化学];

摘要：

Combining computer-assisted drug design and synthetic efforts, we generated compounds with potent and balanced activities toward both D3 dopamine receptor and fatty acid amide hydrolase (FAAH) enzyme. By concurrently modulating these targets, our compounds hold great potential toward exerting a disease-modifying effect on nicotine addiction and other forms of compulsive behavior.

引用

页码：4904 / 4907

页数：4

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