Radioiodinated alpha-p-iodophenyl-N-tert-butylnitrone as a radical detecting agent in vivo.
For in vivo detection of unstable radical species, a novel radioiodinated radical trapping agent, alpha-p-iodophenyl-N-tert-butylnitrone (IPBN), was designed based on the plausible characteristics of alpha-p-hydroxy-m-iodophenyl-N-tert-butylnitrone (HIPBN). Both compounds are iodinated analogs of alpha-phenyl-N-tert-butylnitrone (PBN), but the latter showed low stability in vivo. The present compound IPBN was easily prepared and labeled with radioiodine. It showed very stable characteristics in vitro as well as in vivo, but was easily metabolized and retained at sites of superoxide production.
Fujibayashi
Y
Y
Department of Radiopharmaceutical Chemistry, Fukui Medical School, Japan. yfuji@pharm.kyoto-u.ac.jp
Tajima
N
N
Wada
K
K
Waki
A
A
Sakahara
H
H
Konishi
J
J
Yokoyama
A
A
D000818:Animals; D003497:Cyclic N-Oxides; D004355:Drug Stability; D005609:Free Radicals; D006801:Humans; D007457:Iodine Radioisotopes; D008297:Male; D051379:Mice; D009589:Nitrogen Oxides / Q000493:pharmacokinetics*; D013481:Superoxides / Q000378:metabolism*; D014018:Tissue Distribution; D014407:Tumor Cells, Cultured
D003497:Cyclic N-Oxides; D005609:Free Radicals; D007457:Iodine Radioisotopes; D009589:Nitrogen Oxides; D013481:Superoxides; C029217:phenyl-N-tert-butylnitrone