926652-87-1Relevant academic research and scientific papers
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
Bennacef, Idriss,Haile, Colin N.,Schmidt, Anne,Koren, Andrei O.,Seibyl, John P.,Staley, Julie K.,Bois, Frederic,Baldwin, Ronald M.,Tamagnan, Gilles
, p. 7582 - 7591 (2006)
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.
