摘要：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.
