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International Journal of Biomedical Imaging
Volume 2007 (2007), Article ID 49791, 5 pages
http://dx.doi.org/10.1155/2007/49791
Research Article

In Vivo Evaluation of the Nitroimidazole-Based Thioflavin-T Derivatives as Cerebral Ischemia Markers

Bejing National Laboratory for Molecular Sciences (BNLMS), Department of Applied Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China

Received 10 April 2007; Accepted 5 July 2007

Academic Editor: Wei Liang

Copyright © 2007 Taiwei Chu et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Timely imaging and accurate interpretation of cerebral ischemia are required to identify patients who might benefit from more aggressive therapy, and nuclear medicine offers a noninvasive method for demonstrating cerebral ischemia. Three nitroimidazole-based thioflavin-T derivatives, N-[4-(benzothiazol-2-yl)phenyl]-3-(4-nitroimidazole-1-yl) propanamide (4NPBTA), N-[4-(benzothiazol-2-yl)phenyl]-3-(4-nitroimidazole-1-yl)-N-methylpropanamide (4NPBTA-1), and N-[4-(benzothiazol-2-yl)phenyl]-3-(2-nitroimidazole-1-yl) propanamide (2NPBTA), were radioiodinated and evaluated as possible cerebral ischemia markers. In normal mice, these compounds showed good permeation of the intact blood-brain barrier (BBB), high initial brain uptake, and rapid washout. In gerbil stroke models that had been subjected to right common carotid artery ligation to produce cerebral ischemia, [I131]2NPBTA, uptake in the right cerebral hemisphere decreased more slowly than that of the left, and the right/left hemisphere uptake ratios increased with time. Also, the right/left hemisphere uptake ratios correlated positively with the severity of the stroke. The results showed that [I131]2NPBTA had a specific location in the cerebral ischemic tissue. This represented a first step in finding new drugs and might provide a possible cerebral ischemic marker.