新型葡萄糖类似物^(99)Tc^mN-DGDTC的药代动力学和显像研究  

~99Tc^mN-DGDTC,a New Glucose Metabolic Agent,the Pharmacokinetics and Imaging Results

作　　者：金仲慧[1] 吕忠文[2] 张卫方[1] 张燕燕[1] 盛晓燕[1] 任佳蕾[3] 张俊波[3] 

机构地区：[1]北京大学第三医院,北京100191 [2]吉林大学中日联谊医院 [3]北京师范大学化学系

出　　处：《中国实验诊断学》2011年第7期1069-1072,共4页Chinese Journal of Laboratory Diagnosis

摘　　要：目的探讨[99TcmN]2+间接标记二硫代氨基甲酸脱氧葡萄糖(deoxyglucose dithiocarbamate,DGDTC)药代动力学特点以及在荷瘤模型小鼠和兔的显像效果。方法药代动力学研究:标记后的[99TcmN]-DGDTC化合物经耳缘静脉注射入健康成年新西兰大白兔体内,于特定时间点采血测定放射计数,以专业软件进行药代动力学计算。动物肿瘤模型显像:分别以荷瘤Balb/C小鼠和新西兰大白兔进行。分别移植H22鼠肝癌细胞系和VX2兔肝癌细胞系于10只小鼠和5只兔子皮下,待肿瘤成型后静脉注射99TcmN-DGDTC复合物行显像观察,并均以99Tcm-高锝酸盐显像作为对照研究。扫描方法:采集血流相、血池相和连续静态图像直至注射后2-4 h(小时)。结果药代动力学结果证明99TcmN-DGDTC复合物体内分布为二室模型,有效半衰期为34.05 min。显像结果证明99TcmN-DGDTC复合物能充分显示小鼠和兔肿瘤模型的病变所在,注射后2 h肿瘤区/周围组织放射计数比值大于2。结论药代动力学和显像研究结果充分证实了99TcmN-DGDTC作为新的肿瘤代谢显像剂的可行性。Objective To evaluate the pharmacokinetic characteristics and feasibility of imaging in tumor-bearing mice and rabbits of [99TcmN]2＋ intermediate radiolabelled deoxyglucose dithiocarbamate（DGDTC）.Methods The DGDTC was synthesized and radiolabelled with [99TcmN]2＋ to form the 99 TcmN-DGDTC complex under the guideline of kit.Pharmacokinetics data of healthy rabbits were acquired by collecting radio counts of auricular vein and processed with software DAS2.1.1.Animal tumor model（10 mice with H22 transplanted cancer and 5 rabits with VX2 transplanted cancer） imaging was designed to two groups,99TcmN-DGDTC group and 99Tcm pertechnetate group（as a control）.Scintigraphy was performed with blood flow,blood pool,and static acquisition continuously,till 2-4 hours after injection.Results The pharmacokinetics results were proved to be a two-compartment model,and t1/2 was 34.05 minutes.Scintigraphic results showed 99 TcmN-DGDTC complex could display tumor well in mice and rabbits tumor model.The count ratio of tumor to nontumorous tissue kept above 2 within 2 hours injected,suggesting the well tumor utilizing of 99 TcmN-DGDTC.Conclusion The pharmacokinetics results and scintigraphic findings supported the potential use of 99 TcmN DGDTC as a functional imaging agent.

关 键 词：99Tcm DGDTC SPECT 动物模型 肿瘤 

分 类 号：R96[医药卫生—药理学]