乏氧显像剂^99Tcm-HL91衍生物的制备及其活性评价  

Preparation and Evaluation of ^(99)Tc^m-HL91 Derivatives for Tumor Hypoxia Imaging

作　　者：范文博[1,2] 李黎[1] 张剑英[1] 韩梅[1] 朱霖[1] 

机构地区：[1]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 [2]福建医科大学附属厦门第一医院核医学科,闽南PET中心,福建厦门361003

出　　处：《核化学与放射化学》2009年第1期16-22,共7页Journal of Nuclear and Radiochemistry

基　　金：高等学校博士学科点专项科研基金(20040027011)

摘　　要：为寻找性能优良的乏氧显像剂,设计合成了2种HL91衍生物4,9-二氮-3,10-二甲基十二-烷2,11-二酮肟(TMBAO)和4,9-二氮-3,10-二氧基十二烷-2,11-二酮肟(H2Pab),并进行99Tcm标记。与已知乏氧显像剂99Tcm-HL91进行比较,并对新标记物的体内外活性进行了评价。乏氧细胞实验结果表明:与99Tcm-HL91相比,99Tcm-TMBAO和99Tcm-H2Pab具有一定的乏氧选择性;荷瘤小鼠体内生物分布数据显示,尽管两种新的99Tcm标记物在肝脏的摄取比99Tcm-HL91低,但其乏氧选择性也同时显著降低。In order to find the optimum hypoxia imaging agent, two derivatives of HL91-4, 9- diaza-3, 10-dimethyl-dodeeane-2, 11-dione dioxime （TMBAO） and N, N＇-bis （2-hydroxyimino propionyl）-1, 4-diaminobutane（H2Pab） were synthesized and labeled with 99Tern. Evaluation of these complexes as tumor hypoxia markers were performed both in vitro and in vivo compared with 99Tcm-HL91-a putative hypoxic tracer. The tumor cell experiment and the biodis- tribution in mice bearing EMT-6 tumor show that the two derivatives-99 Tcm-TMBAO and 99Tcm-H2Pab have less hypoxic selectivity than 99Tem-HL91 in despite of their lower liver up- take.

关 键 词：99Tcm-HL91 99Tcm-TMBAO 99Tcm-H2Pab 乏氧 生物分布 

分 类 号：R981.2[医药卫生—药品] TQ463.7[医药卫生—药学]