Potent cannabinergic indole analogues as radioiodinatable brain imaging agents for the CB1 cannabinoid receptor

…, JR Deschamps, JL Flippen-Anderson…

文献索引：Deng, Hongfeng; Gifford, Andrew N.; Zvonok, Alexander M.; Cui, Guangjian; Li, Xiuyan; Fan, Pusheng; Deschamps, Jeffrey R.; Flippen-Anderson, Judith L.; Gatley, S. John; Makriyannis, Alexandros Journal of Medicinal Chemistry, 2005 , vol. 48, # 20 p. 6386 - 6392

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被引用次数: 42

摘要

A series of novel aminoalkylindoles was synthesized in an effort to develop compounds that are potent agonists at the CB1 cannabinoid receptor and that are also easily labeled with radioisotopes of iodine for biochemical and imaging studies. 2-Iodophenyl-[1-(1- methylpiperidin-2-ylmethyl)-1 H-indol-3-yl] methanone (8, AM2233) had a very high affinity for the rat CB1 receptor, with most of the affinity residing with the (R)-enantiomer. ...