Kung H F, Yu C C, Billings J, Molnar M, Blau M
J Med Chem. 1985 Sep;28(9):1280-4. doi: 10.1021/jm00147a028.
In developing new brain perfusion imaging agents for single photon emission computed tomography (SPECT), five 99mTc-labeled neutral bis(aminoethanethiol) (BAT) derivatives capable of crossing the blood-brain barrier are reported. The five ligands are prepared by two versatile synthetic methods that can specifically introduce substituents on one of the carbons between two nitrogens. These ligands formed stable and neutral complexes with the reduced 99mTc, using either Sn(II) or sodium borohydride to reduce sodium [99mTc]pertechnetate. The biodistribution in rats was evaluated with [125I]iodoantipyrine, a freely diffusible tracer, as the internal reference. Compounds with a free hydroxyl group, 6 and 15, showed lower brain uptake. High initial brain uptake was observed for compounds 10 and 14, 1.28 and 2.30% dose/organ, respectively. Compounds of this type may be used as a basis for future structural modification to improve brain uptake and retention.
在开发用于单光子发射计算机断层扫描（SPECT）的新型脑灌注显像剂时，报道了五种能够穿过血脑屏障的99mTc标记的中性双（氨基乙硫醇）（BAT）衍生物。这五种配体通过两种通用的合成方法制备，这两种方法可以在两个氮原子之间的一个碳原子上特异性引入取代基。这些配体与还原态的99mTc形成稳定的中性络合物，使用Sn（II）或硼氢化钠还原高锝酸钠[99mTc]。以可自由扩散的示踪剂[125I]碘安替比林作为内参，评估了大鼠体内的生物分布。具有游离羟基的化合物6和15显示出较低的脑摄取。化合物10和14的初始脑摄取较高，分别为1.28%和2.30%剂量/器官。这类化合物可用作未来结构修饰的基础，以提高脑摄取和滞留。
