中文摘要：

合成了一种含有（2-甲氧基苯基）哌嗪（MPP）活性基团的4-[（2-甲氧基苯基）哌嗪基]-二硫代甲酸盐（MPPDTF），式中MPP基团是与5-HT1A-脑受体具有高亲和性的药效团．通过元素分析、红外光谱（IR）、核磁（^1H NMR）及质谱（EI—MS）等表征确认了配体的结构．^99mTcN核标记配合物按两步法制备：先由药盒法制得中间体（[^99mTc≡N]int^2＋），然后通过配体交换反应制得最终标记配合物（^99mTcN（MPPDTF）2）．配体交换反应条件在配体用量、反应pH值、反应温度以及反应时间等方面经过细致的优化，在最佳标记条件下可制得放射化学纯度大于98％的最终配合物．中间体和最终配合物的制备均经过TLC和HPLC鉴定．^99mTcN（MPPDTF）。配合物为中性、脂溶性配合物（P=49．5±3．5，n=3），在室温下放置6h以上放化纯无明显变化．

英文摘要：

The 5-HT1A receptor-binding domain, （2-methoxyphenyl）-piperazinyl （MPP）, is linked with a chelating group dithioformate （DTF） to give a bidentate ligand 4-[（2-methoxyphenyl）piperazin-l-yl]-dithioformate （MPPDTF）. The desired molecule structure is conformed by elemental analysis, IR, ^1H NMR, and EI-MS, respectively. Radiolabeling conditions of ^99mTcN-MPPDTF are optimized and the complex is obtained by using two-step procedure that leads to the formation of the complex with high radiochemical purity （〉98% by HPLC）. ^99mTcN-MPPDTF is a neutral and lipophilic complex, it is conformed by paper electrophoresis and octanol/water partition coefficient （P = 49.5 ± 3. 5, n=3）, respectively. The in vitro and in vivo specific binding affinity of this radioligand to 5-HT1A receptor will be tested in the near future.