锝-99m对碘苯乙基二氨基二硫醇(DADT-IPE): SPECT潜在的脑灌注显像剂

K. Shiba , H. Mori , H. Matsuda , K. Hisada
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引用次数: 1

摘要

合成了n -异丙基-对碘安非他明(IMP)类似物n -对碘苯乙二氨基二硫醇(DADT-IPE),并以氯化亚锡为还原剂与99mTc络合。用高效液相色谱法从99mTc-DADT-IPE中分离出两个配合物a和b。竞争抑制实验表明,DADT-IPE (70 μM)的IC50值与IMP (49 μM)相似。Biodistribution研究之一的复合物[99 mtc-dadt-ipe (a)]的老鼠显示0.65%的大脑中示踪剂的注入剂量仍在静脉注射后5分钟,剩下0.53%的剂量在60分钟post-injection大脑,而相应的值对于其他复杂[99 mtc-dadt-ipe (b)] 0.34%剂量在大脑中5分钟和0.28%剂量在60分钟post-injection大脑。99mTc-DADT-IPE(a)在大鼠脑内的清除半衰期大于5 h,表明99mTc-DADT-IPE(a)具有适合脑灌注成像的特性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Technetium-99m p-iodophenethyldiaminodithiol (DADT-IPE): Potential brain perfusion imaging agent for SPECT

A new ligand, an N-p-iodophenethyl diaminodithiol (DADT-IPE), an anlog of N-isopropyl-p-iodoamphetamine (IMP), was synthesized and subsequently complexed with 99mTc, using stannous chloride as a reducing agent. Two complexes (a and b) were separated from 99mTc-DADT-IPE by high performance liquid chromatography (HPLC). Competitive inhibition studies showed that the IC50 value of DADT-IPE (70 μM) was similar to that of IMP (49 μM). Biodistribution studies of one of the complexes [99mTc-DADT-IPE(a)] in rats showed that 0.65% of the injected dose of the tracer remained in the brain at 5 min after intravenous injection, with 0.53% of the dose remaining in the brain at 60 min post-injection, whereas the corresponding values for the other complex [99mTc-DADT-IPE(b)] were 0.34% dose in the brain at 5 min and 0.28% dose in the brain at 60 min post-injection. The half-life for clearance of 99mTc-DADT-IPE(a) from rat brain was found to be more than 5 h. These results suggested that 99mTc-DADT-IPE(a) has characteristics which are suitable for cerebral perfusion imaging.

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