Synthesis and biological evaluation of radioiodinated 2NUBTA as a cerebral ischemia marker

Bioorg Med Chem Lett. 2009 Feb 1;19(3):658-61. doi: 10.1016/j.bmcl.2008.12.052. Epub 2008 Dec 24.

Abstract

N-[4-(Benzothiazol-2-yl)phenyl]-11-(2-nitroimidazole-1-yl)undecanamide (2NUBTA) was synthesized and radiolabeled with iodine-131. In vitro evaluation of the [(131)I]2NUBTA using murine sarcoma S180 cells showed increase in radioactivity in hypoxic cells up to 4h, while it was not in aerobic cells. Its potential as a cerebral ischemia marker was evaluated using gerbil stroke models that had been subjected to right common carotid artery ligation to produce cerebral ischemia. The uptake in the right cerebral hemisphere decreased slowly than that of the left and the right/left hemisphere uptake ratios increased with time going on. It indicated that [(131)I]2NUBTA might be a possible cerebral ischemia marker.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzothiazoles
  • Biomarkers
  • Blood-Brain Barrier
  • Brain Ischemia / diagnosis*
  • Brain Ischemia / diagnostic imaging*
  • Cell Line, Tumor
  • Humans
  • Hypoxia
  • Iodine Radioisotopes / pharmacology*
  • Mice
  • Models, Chemical
  • Nitroimidazoles / chemical synthesis*
  • Nitroimidazoles / pharmacology*
  • Radionuclide Imaging
  • Temperature
  • Thiazoles / chemical synthesis*
  • Thiazoles / chemistry
  • Thiazoles / pharmacology*

Substances

  • Benzothiazoles
  • Biomarkers
  • Iodine Radioisotopes
  • N-(4-(benzothiazol-2-yl)phenyl)-11-(2-nitroimidazole-1-yl)undecanamide
  • Nitroimidazoles
  • Thiazoles
  • thioflavin T