Synthesis of quinolinyl and isoquinolinyl phenyl ketones as novel agonists for the cannabinoid CB2 receptor

被引：75
作者：
Reux, Bastien [1 ]
Nevalainen, Tapio [2 ]
Raitio, Katri H. [2 ]
Koskinen, Ari M. P. [1 ]
机构：
[1] Aalto Univ, Organ Chem Lab, FIN-02015 Espoo, Finland
[2] Univ Kuopio, Dept Pharmaceut Chem, FIN-70211 Kuopio, Finland
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 13期
基金：
芬兰科学院;
关键词：
Cannabinoid receptor; CB2; Quinoline; Isoquinoline; IN-VIVO; PHARMACOLOGY; PROGRESSION; LIGANDS; MODEL;
D O I：
10.1016/j.bmc.2009.05.013
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A series of quinolinyl and isoquinolinyl phenyl ketones was synthesized and their CB2 receptor-dependent G-protein activities were determined using the [S-35] GTP gamma S binding assay. Both quinoline and isoquinoline derivatives exhibited similar CB2 receptor agonist activity, the most potent ligands being the 2-(Me2N)-phenyl substituted derivatives, which were also full agonists at the CB2-receptor. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4441 / 4447
页数：7
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