喹啉基和异喹啉基苯基酮作为大麻素CB2受体新型激动剂的合成。
Synthesis of quinolinyl and isoquinolinyl phenyl ketones as novel agonists for the cannabinoid CB2 receptor.
作者信息
Reux Bastien, Nevalainen Tapio, Raitio Katri H, Koskinen Ari M P
机构信息
Laboratory of Organic Chemistry, Helsinki University of Technology, Finland.
出版信息
Bioorg Med Chem. 2009 Jul 1;17(13):4441-7. doi: 10.1016/j.bmc.2009.05.013. Epub 2009 May 12.
A series of quinolinyl and isoquinolinyl phenyl ketones was synthesized and their CB(2) receptor-dependent G-protein activities were determined using the [(35)S]GTPgammaS binding assay. Both quinoline and isoquinoline derivatives exhibited similar CB(2) receptor agonist activity, the most potent ligands being the 2-(Me(2)N)-phenyl substituted derivatives, which were also full agonists at the CB(2)-receptor.
合成了一系列喹啉基和异喹啉基苯基酮，并使用[³⁵S]GTPγS结合试验测定了它们CB(2)受体依赖性G蛋白活性。喹啉和异喹啉衍生物均表现出相似的CB(2)受体激动剂活性，最有效的配体是2-(二甲基氨基)-苯基取代的衍生物，它们也是CB(2)受体的完全激动剂。
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