Synthesis and biological evaluation of radioiodinated 2NUBTA as a cerebral ischemia marker.
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.
Chu
Taiwei
T
Bejing National Laboratory for Molecular Sciences, Department of Applied Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China. twchu@pku.edu.cn
Li
Zejun
Z
Wang
Xiangyun
X
D000818:Animals; D052160:Benzothiazoles; D015415:Biomarkers; D001812:Blood-Brain Barrier; D002545:Brain Ischemia / Q000175:diagnosis* / Q000000981:diagnostic imaging*; D045744:Cell Line, Tumor; D006801:Humans; D000860:Hypoxia; D007457:Iodine Radioisotopes / Q000494:pharmacology*; D051379:Mice; D008956:Models, Chemical; D009593:Nitroimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D011877:Radionuclide Imaging; D013696:Temperature; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D052160:Benzothiazoles; D015415:Biomarkers; D007457:Iodine Radioisotopes; C540260:N-(4-(benzothiazol-2-yl)phenyl)-11-(2-nitroimidazole-1-yl)undecanamide; D009593:Nitroimidazoles; D013844:Thiazoles; C009462:thioflavin T