Synthesis and receptor binding studies of halogenated N,N-dialkylel-(2-phenyl-1H-indol-3-yl)glyoxylamides to visualize peripheral benzodiazepine receptors with SPECT or PET.
Synthesis and receptor binding studies of halogenated N,N-dialkylel-(2-phenyl-1H-indol-3-yl)glyoxylamides to visualize peripheral benzodiazepine receptors with SPECT or PET.
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卤化 N,N-二烷基-(2-苯基-1H-吲哚-3-基)乙醛酰胺的合成和受体结合研究，通过 SPECT 或 PET 可视化外周苯二氮卓受体。
DOI：
10.1016/j.bmc.2006.07.001
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发表时间：
2006
影响因子：
3.5
通讯作者：
Tamagnan,Gilles
中科院分区：
文献类型：
--
作者：
Bennacef,Idriss;Haile,ColinN;Schmidt,Anne;Koren,AndreiO;Seibyl,JohnP;Staley,JulieK;Bois,Frederic;Baldwin,RonaldM;Tamagnan,Gilles
A library of halogenated 2-arylindolyl-3-oxocarboxamides was prepared to develop radioligands to visualize cerebral PBR by SPECT and PET imaging. In vitro evaluation showed that most of the synthesized compounds were selective,high-affinity PBR ligands with adequate lipophilicity (logD7.4in the range of 1.6–2.4). The iodinated derivative 11 (Ki=2.6nM) and the fluorinated analog 26 (Ki=6.2nM) displayed higher affinity than reference compounds.
