Synthesis and biological evaluation of ^(99m)Tc-HEDTA/HYNIC-MPP4 complex for 5-HT_(1A) receptor imaging  

作　　者：FAN WeiWei LIN Yan ZHANG XianZhong PANG Yan MA Cong TANG ZhiGang ZHANG JunBo WANG XueBin 

机构地区：[1]Key Laboratory of Radiopharmaceuticals,Ministry of Education,College of Chemistry,Beijing Normal University,Beijing 100875,China

出　　处：《Science China Chemistry》2009年第5期590-598,共9页中国科学(化学英文版)

基　　金：Supported by the National Natural Science Foundation of China(Grant No.20401004);the Analysis and Test fund of Beijing Normal University

摘　　要：5-HT_(1A)receptor is associated with a variety of pathophysiology of neuropsychiatric disorders.Accordingly,we have synthesized a new 5-HT_(1A) receptor ligand(HYNIC-MPP4)and labeled it with^(99m)Tc using N-(2-hydroxyethyl)ethylenediaminetriacetic acid(HEDTA)as coligand.^(99m)Tc-HEDTA/HYNIC-MPP4 was prepared under pH 6 at room temperature.Biodistribution of^(99m)Tc-HEDTA/HYNIC-MPP4 in normal mice showed that this complex had moderate brain uptake(0.60%ID·g^(-1)at 2 min p.i.)and good retention.The hippocampus had the highest radioactivity uptake at 2 min p.i.(1.84%ID·g^(-1)).The ratio of Hipp/CB was 3.1 at 2 min p.i.and increased to 4.4 at 60 min p.i.After blocking with 8-hydroxy-2-(dipropylamino)tetralin,the uptake of hippocampus was decreased significantly from 1.84%ID·g^(-1) to 0.53%ID·g^(-1) at 2 min p.i.,while the cerebellum had no significant decrease.This^(99m)Tc complex could be a potent agent for 5-HT_(1A) receptor imaging.

关 键 词：5-HT_(1A)receptor ^(99m)Tc N-{4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl}-3-(6-hydrazinyl)pyridyl carboxamide(HYNIC-MPP4) BIODISTRIBUTION 

分 类 号：R817[医药卫生—影像医学与核医学]