Lever S Z, Burns H D, Kervitsky T M, Goldfarb H W, Woo D V, Wong D F, Epps L A, Kramer A V, Wagner H N
J Nucl Med. 1985 Nov;26(11):1287-94.
A new ligand (N-piperidinylethyl-DADT, 5) has been prepared which forms two complexes with 99mTc when stannous chloride is used as a reducing agent for [99mTc] pertechnetate. Biodistribution studies of one of the complexes in mice showed that 2.2% of the injected dose of the tracer was in the brain at 5 min postintravenous injection with 0.53% of the dose remaining in the brain at 30 min postinjection. Brain-to-blood ratios at these times were 5.3 and 3.0, respectively. Biodistribution studies of the other complex showed similar behavior with a slightly lower initial uptake by and faster clearance from the brain. Imaging studies of the more promising of the two complexes were conducted in a monkey and a baboon. In both cases, rapid uptake of the tracer in the brain was observed and clear brain images were obtained. Time-activity curves showed peak uptake in the brain at approximately 5 to 7 min postintravenous injection followed by a plateau of about 11 min. The half-lives for clearance of the tracer from the brains of the monkey and baboon were found to be 63 and 58 min, respectively. These results suggest that this tracer may be useful for brain imaging in humans.
一种新的配体（N-哌啶基乙基-DADT，5）已被制备出来，当氯化亚锡用作高锝[99mTc]酸盐的还原剂时，它能与99mTc形成两种配合物。对其中一种配合物在小鼠体内的生物分布研究表明，静脉注射后5分钟，示踪剂注射剂量的2.2%存在于脑中，注射后30分钟，脑中仍残留0.53%的剂量。这些时间点的脑血比分别为5.3和3.0。对另一种配合物的生物分布研究显示出类似的行为，只是其在脑中的初始摄取略低且从脑中清除更快。对这两种配合物中更有前景的一种进行了在猴子和狒狒身上的成像研究。在这两种情况下，均观察到示踪剂在脑中快速摄取，并获得了清晰的脑图像。时间-活性曲线显示，静脉注射后约5至7分钟脑摄取达到峰值，随后有大约11分钟的平台期。发现示踪剂从猴子和狒狒脑中清除的半衰期分别为63分钟和58分钟。这些结果表明，这种示踪剂可能对人类脑成像有用。
