一种新型潜在^(99m)TcN核标记5-HT_(1A)脑受体显像剂的制备研究  

SYNTHESIS AND RADIOLABELING OF ^(99m)Tc-NITRIDO COMPLEX WITH 4-[(2-METHOXYPHENYL)PIPERAZIN-1-YL]-DITHIOFORMATE AS A POTENTIAL 5-HT_(1A) RECEPTOR IMAGING AGENT

作　　者：张现忠[1] 周潘旺[1] 刘姣姣[1] 黄艳[1] 顾婷[1] 陈妍伶[1] 王学斌[1] 

机构地区：[1]北京师范大学放射性药物教育部重点实验室北京师范大学化学学院,北京100875

出　　处：《北京师范大学学报（自然科学版）》2006年第4期395-400,共6页Journal of Beijing Normal University(Natural Science)

基　　金：国家自然科学基金资助项目(20401004)

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(1HNMR)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]i2nt+),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)2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6 h以上放化纯无明显变化.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.

关 键 词：5-HT1A受体 4-[(2-甲氧基苯基)哌嗪基]-二硫代甲酸盐 ^99mTcN核配合物 显像剂 

分 类 号：TQ573.8[化学工程—精细化工]