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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| Authors: | Bennacef Idriss Haile Colin N Schmidt Anne Koren Andrei O Seibyl John P Staley Julie K Bois Frederic Baldwin Ronald M Tamagnan Gilles |
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| Institution: | Yale School of Medicine, VA Connecticut HCS (116A2), West Haven, CT 06516, USA. |
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| Abstract: | 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 (log D7.4 in the range of 1.6-2.4). The iodinated derivative 11 (Ki = 2.6 nM) and the fluorinated analog 26 (Ki = 6.2 nM) displayed higher affinity than reference compounds. |
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