Efange S M, Kung H F, Billings J, Guo Y Z, Blau M
J Nucl Med. 1987 Jun;28(6):1012-9.
In an effort to develop new clinically useful technetium-99m bis(aminoethanethiol) ([99mTc]BAT) complexes for the evaluation of regional cerebral perfusion, two new BAT ligands containing amines in the sidechain were synthesized and subsequently complexed with 99mTc to yield the target complexes: [99mTc]DEA and [99mTc]TMPDA. Each complex was obtained as mixtures of two isomers, syn and anti, which were separated chromatographically. In biodistribution studies, both isomers of [99mTc]TMPDA showed little uptake in the brain. In contrast, the brain uptake values at 2 and 15 min for [99mTc]DEA-anti were 0.99 and 0.26, whereas, the corresponding values for DEA-syn were 2.27, 0.64% dose/organ, respectively. Autoradiographic studies (in rats) using both isomers of [99mTc]DEA show a fixed regional distribution and a higher concentration of radioactivity in the gray matter relative to the white matter. Planar imaging using [99mTc]DEA-syn clearly demonstrates localization of the complex in the brain with a T 1/2 of 41 min, suggesting some potential for use with single photon emission computed tomography.
为了开发新型具有临床应用价值的锝-99m双（氨基乙硫醇）（[99mTc]BAT）配合物用于评估局部脑灌注，合成了两种侧链含胺的新型BAT配体，随后与99mTc络合得到目标配合物：[99mTc]DEA和[99mTc]TMPDA。每种配合物均以顺式和反式两种异构体的混合物形式获得，并通过色谱法进行分离。在生物分布研究中，[99mTc]TMPDA的两种异构体在脑中的摄取都很少。相比之下，[99mTc]DEA-反式在2分钟和15分钟时的脑摄取值分别为0.99%和0.26%，而DEA-顺式的相应值分别为2.27%和0.64%（剂量/器官）。使用[99mTc]DEA的两种异构体进行的（大鼠）放射自显影研究显示出固定的区域分布，且灰质中的放射性浓度相对于白质更高。使用[99mTc]DEA-顺式进行的平面成像清楚地显示了该配合物在脑中的定位，其半衰期为41分钟，表明其在单光子发射计算机断层扫描方面具有一定的应用潜力。
