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目的 研究多巴胺转运蛋白 (DAT)显像剂99Tcm 2 β [N ,N’ 双 (2 巯乙基 )乙撑二胺基 ]甲基 ,3β (4 氯苯基 )托烷 (TRODAT 1)用于帕金森病 (PD)早期诊断的价值。 方法 制备99Tcm TRODAT 1,用 2 β 羧甲基 ,3β (4 碘苯基 )托烷 (β CIT)阻断DAT后 ,观察大鼠脑内分布、兔血药清除动力学、异常毒性实验、正常及PD模型鼠的放射自显影图并对志愿者进行显像。结果 制备的99Tcm TRODAT 1放化纯大于 90 % ,室温下放置 6h稳定 ;用 β CIT阻断后大鼠纹状体的特异性摄取即纹状体与小脑放射性计数差除以小脑放射性计数为 0 .12 (对照组为 3.45 ) ,表明 β CIT对99Tcm TRODAT 1有明显的竞争抑制作用。血药清除动力学研究表明它的分布半衰期T1/2 (α) =1.2min ,消除半衰期T1/2 (β) =36 8min。模型鼠的放射自显影结果表明纹状体的特异摄取随着给药 (神经毒素 )总量的增加而减少 ,并有良好的线性关系 (r =- 0 .9792 )。正常猴断层显像在 3个断面上基底节均有明显高于周围组织的摄取 ,单侧PD模型猴显像示健侧纹状体与小脑的比值 (1.5 6 )明显高于损毁侧比值 (0 .94)。志愿者脑断层图像清晰 ,患侧纹状体对99Tcm TRODAT 1摄取较正常侧减低 ,其显像结果分析与临床表现相吻合。结论 99Tcm TRODAT 1制备方便 ,体外稳定
Objective To study the effect of dopamine transporter (DAT) imaging agent 99Tcm 2 β [N, N ’bis (2mercaptoethyl) ethylenediamino] methyl and 3β (4chlorophenyl) tropane The value of early diagnosis of Parkinson’s disease (PD). Methods The 99 Tcm TRODAT 1 was prepared and blocked with 2 β carboxymethyl group and 3 β (4 iodophenyl) tropane (β CIT) to observe the distribution in the brain, the kinetics of clearance of blood serum in rabbits, abnormal toxicity test, normal And PD model mice autoradiogram and volunteer imaging. Results The radiochemical purity of 99 Tcm TRODAT 1 was more than 90%, which was stable at room temperature for 6 h. The specific uptake of striatum in rat striatum after blocking with β CIT was significantly lower than that of striatum and cerebellum .12 (control group, 3.45), indicating that β CIT has a significant competitive inhibition of 99 Tcm TRODAT 1. The kinetics of plasma clearance showed that its distribution half-life T1 / 2 (α) = 1.2min, elimination half-life T1 / 2 (β) = 368min. Autoradiographs of model mice showed that the specific uptake of striatum decreased with increasing total amount of neurotoxin and had a good linear relationship (r = -0.9792). Normal monkey tomography in the three sections of the basal ganglia were significantly higher than the surrounding tissue uptake, monophasic PD model monkey showed the ratio of the contralateral corpus striatum and cerebellum (1.5 6) was significantly higher than the damage ratio ( 0 .94). Cerebral infarction images were clear in the volunteers, and the incidence of 99Tcm TRODAT 1 in the affected side of the striatum was lower than that in the normal side. The imaging results were consistent with clinical manifestations. Conclusion 99Tcm TRODAT 1 is easy to prepare and stable in vitro