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

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.

• Authors: Taiwei Chu, Zejun Li, Xiangyun Wang
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 19 Issue 3 Pg. 658-61 (Feb 01 2009) ISSN: 1464-3405 [Electronic] England
• PMID: 19121583 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

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

Topics

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