摘要
目的探讨99Tcm-RGD-4CK在健康日本大耳兔体内的示踪动力学。方法采用预锡化法99Tcm直接标记RGD-4CK。静脉注射99Tcm-RGD-4CK37MBq(0.5ml),在注射后1.5~240min时间内分10个时相点采血并称重,测定血样品放射性计数,结果经参考源衰减校正,最后换算为kBq/ml血液。血样放射性活度数据应用DAS软件处理,结合αvβ3受体在正常体内实际表达情况进行室模型判断,并得出相应的示踪动力学参数。结果99Tcm-RGD-4CK的标记率为(96·86±1.24)%,比活度为(13.01±0.17)TBq/mmol。99Tcm-RGD-4CK在正常家兔体内符合二室模型示踪动力学过程(权重数为1/C)。分布相半衰期(T1/2α)为(4.19±2.17)min,消除相半衰期(T1/2β)为(69.32±0.00)min,转运速率常数K10、K12与K21分别为(0.013±0.002)、(0.138±0.139)、(0.095±0.063)/min,清除率(CL)为(2.00±1.00)ml/min。结论99Tcm-RGD-4CK制备方法简便,标记率高,无需分离纯化而直接应用;99Tcm-RGD-4CK在正常家兔体内的示踪动力学符合权重数为1/C的二室模型。
Objective To investigate the tracer kinetics of ^99Tc^m-RGD-4CK in normal rabbit. Methods RGD-4CK was labeled directly with ^99Tc^m by the ＂pretinning＂ method. After injection of the ^99Tc^m-RGD-4CK solution in 37 MBq （0.5 ml） via auris vein, blood was sampled from the opposite auris vein for 10 phases during 1.5 to 240 min and weighted. Radioactivity of blood samples were measured by γ scintillation counter and corrected by referenced source of ^99Tc^m-RGD-4CK, the results was finally expressed as kBq per milliliter blood. The data were processed by computer with DAS program, the compartment model was judged in combination of the actual expression of αvβ3 receptor in normal body and the relevant tracer kinetics parameters were obtained. Results The labeling efficiency and specific activity of ^99Tc^m-RGD-4CK was （96.86 ± 1.24）% and （13.01 ±0.17） TBq/mmol respectively. The tracer kinetics process of ^99Tc^m-RGD-4CK matched the two compartment model in normal rabbit （Weighted = 1/C）. The T1/2α of ^99Tc^m-RGD4CK was （4.19 ±2.17） min in blood and T1/2β was （69.32 ±0.00） min, the K10, K12 and K21 was （0.013 ±0. 002）/min, （0. 138 ±0. 139）/min and （0. 095 ±0. 062）/min respectively, and CL was （2.05 ± 0.41 ） ml/min. Oonelusion The preparation of ^99Tc^m-RGD-4CK is simple, labeling efficiency is high and labeling product can be used directly without separation and purification. The tracer kinetics of ^99Tc^m-RGD-4CK fits the two compartment model （Weighted = 1/C） in normal rabbit.
出处
《第三军医大学学报》
CAS
CSCD
北大核心
2006年第22期2230-2233,共4页
Journal of Third Military Medical University
基金
国家自然科学基金资助项目(30370425)
重庆市科委攻关课题(2002)~~
