摘要
目的 评价1 2 5 I 甲基 3β (4 碘苯基 )托烷 2 β 羧酸甲基脂 (β CIT)在体内和脑内的结合特性。方法 应用过氧乙酸标记法和氯胺 T法进行1 2 5 I β CIT标记 ,并进行动物体内分布特性研究。 结果 标记率分别为 (5 3 4± 7 9) %和 (88 4± 3 49) %。小鼠静脉注射1 2 5 I β CIT后 ,放射性主要浓聚在纹状体等脑区 ,其峰值摄取出现在药物注射后 2h。GBR12 90 9显著抑制纹状体内1 2 5 I β CIT的摄取 ,而clomipramine则显著抑制大脑皮层和海马内1 2 5 I β CIT的摄取。大鼠整体放射自显影表明 ,1 2 5 I β CIT主要通过肝胆途径代谢。结论 碘标 β
Objective To prepare and label the 125 I β CIT and study its biological distribution in animal Methods 125 I β CIT was prepared by the peracetic acid method and the chloramine T method, and dopamine transporter (DAT) binding properties of 125 I β CIT were examined by in vivo biodistribution and inhibition studies in mice and whole body autoradiography in rats Results The radiolabeling yields of the peracetic acid and the chloramine T methods were (53 4±7 9)% and (88 4±3 49)%, respectively Following intravenous injection in mice, 125 I β CIT showed high accumulation in striatum, time to peak level uptake was 2 h after injection GBR12909 significantly inhibited 125 I β CIT binding in striatum, while clomipramine significantly inhibited 125 I β CIT binding in hippocampus and cerebral cortex The rat whole body autoradiography showed that the clearance of the tracer occurred through the hepatobiliary route Conclusions The results indicate β CIT is an agent suitable for DAT imaging and can be used for the study of Parkinson's disease
出处
《中华核医学杂志》
CAS
CSCD
北大核心
2000年第3期117-119,共3页
Chinese Journal of Nuclear Medicine
