New brain perfusion imaging agents based on 99mTc-bis(aminoethanethiol) complexes: stereoisomers and biodistribution.
New brain perfusion imaging agents based on 99mTc-bis(aminoethanethiol) complexes: stereoisomers and biodistribution.
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基于 99mTc-双（氨基乙硫醇）复合物的新型脑灌注显像剂：立体异构体和生物分布。
DOI：
10.1021/jm00122a024
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发表时间：
1989
影响因子：
7.3
通讯作者：
Calabrese,JC
中科院分区：
文献类型：
--
作者：
Kung,HF;Guo,YZ;Yu,CC;Billings,J;Subramanyam,V;Calabrese,JC
0硅胶-丙酮。6硅胶-丙酮：二氯甲烷（1:2）。c柱：反相Hamilton PRP-1。溶剂：乙腈- 3,3 -二甲基戊二酸酯缓冲液pH 7.0, 0.1 mM（85: 15）。流量：1ml /min。等（NEP-DADT） 17 ' 22（方案一）。两种类型的碳和氮取代的BAT衍生物与TcmO络合后形成非对映体。在大鼠体内的生物分布数据（剂量/脑内器官摄取百分比）显示异构体之间存在明显差异；syn异构体在大鼠和猴子中表现出更高的吸收和保留。在不断努力开发新的99”t标记脑灌注显像剂，中性和脂溶性”™Tc配合物的bat含有N'-苄基哌嗪基（BPA）侧链制备。由于手性中心的存在，BPA-BAT配体（外消旋混合物）也有望呈现出两种类型的Tc和Tc配合物，即顺式和反式异构体。本文报道了“Tc-BPA-BAT”复合物的制备、结构鉴定及其在大鼠体内的生物分布。配体的合成是通过前面报道的相应的BAT单胺衍生物的程序来实现的。21,22在这些步骤的基础上，生成了外消旋配体BPA-BAT。通过外消旋配体与tc - snn -葡萄糖庚酸酯（方案II）交换反应制备无载体添加的Tc-BPA-BAT配合物。正反同分异构体的比例约为1:1
0 Silica gel-acetone. 6Silica gel-acetone: dichloromethane (1: 2). c Column: reverse-phase Hamilton PRP-1. Solvent: acetonitrile-3, 3-dimethylglutarate buffer pH 7.0, 0.1 mM (85: 15). Flow rate: 1 mL/min. and others (NEP-DADT) 17’22 (Scheme I). Both types of the carbon-and nitrogen-substituted BAT derivatives form diastereomers after complexation with TcmO. The bio-distribution data in rats (% dose/organ uptake in brain) showed a distinctive disparity between the isomers; the syn isomer showed higher uptake and retention in rats and monkeys. In a continuous effort to develop new 99 “Tclabeled brain perfusion imaging agents, neutral and lip-id-soluble"™ Tc complexes ofBAT containing an N'-benzylpiperazinyl (BPA) side chain were prepared. Due to the presence of a chiral center, the BPA-BAT ligand (racemic mixture) is also expected to show two types of"“Tc and" Tc complexes, syn and anti isomers. In this paper, the preparation and structural identification of the" Tc-BPA-BAT complexes and the in vivo biodistribution in rats are reported.Chemistry The ligand synthesis is achieved by a procedure reported earlier for the corresponding monoamine derivatives of BAT. 21, 22 Based on these steps, a racemic ligand BPA-BAT is produced. The no-carrier added"“Tc-BPA-BAT com-plexes were prepared by an exchange reaction betweenthe racemic ligand and"” Tc-Snn-glucoheptonate (Scheme II). The syn and anti isomers (approximately 1: 1 ratio) were