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1. 中山医科大学附属第一医院!广州5100802
2. 广州分析测试中心!广东测试分析研究所广州
3. 中山医科大学,广州,510080
Published:01 May 2000
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[1]胡平,周治发,林展江,李光宪,胡笑克.~(125)I-β-CIT动物体内生物学分布研究[J].核技术,2000(05):289-293.
125I-β-CIT Biodistribution Study in animals[J]. Nuclear techniques, 2000, (5): 289-293.
[1]胡平,周治发,林展江,李光宪,胡笑克.~(125)I-β-CIT动物体内生物学分布研究[J].核技术,2000(05):289-293. DOI:
125I-β-CIT Biodistribution Study in animals[J]. Nuclear techniques, 2000, (5): 289-293. DOI:
了解多巴胺转运体显像剂
125
I-β-CIT在体内的生物学分布情况,为其临床应用提供客观依据。采用Iodogen标记法制备
I-β-CIT,用HPLC进行分离纯化与鉴定,体内生物学分布用NIH小鼠,脑放射性自显影用SD大鼠。结果表明;
I-β-CIT标记率为84%,放化纯度大于98%;NIH小鼠血液清除,12h内符合二室模型(α=3.87,β=0.162;T
1/2α
=0.179;T
1/2β
=4.276);24h为三室模型(Pi=5.28,α=0.403,β=0.040,T
1/2Pi
=0.131,T
=1.719,T
=17.298);脑内摄取注射后1h达高峰(9.1%± 1.0%),关键器官肝、肺、脾、肾也具有较高的摄取[(9.88±1.43)-(16.29±1.72)],除肝外,其它器官均显示了较快的清除(T
1/2
<4h;甲状腺摄取低,提示标记物体内稳定。SD大鼠放射性自显影显示;纹状体摄取好,纹状体/大脑皮质比值在注射后20h达高峰。说明
I-β-CIT在体内具有较好的稳定性和高的纹状体摄取率,可得到较高质量的SPECT图像,最佳采?
The purpose of this artical is to study the preparation and biodistribution in animal of dopamine transporter imaging agent
125
I- β-CIT. β-CIT was
I radioiodinated with odogen method
the dynamic distribution of
I-β-CIT in brain and critical organs were studied with SD rat (atuoradiography) and NIH mice respectively. The radiolabelling yield of
I-β-CIT was 84%
the radiochemical purity was better than 98%. Blood clearance could be explained by two-compartment model with a duration of 12h
(α = 3.87
T
1/2α
=0.179
β =0.162
1/2β
=4.276) and three-compartment model in 24h
(Pi= 5.28
1/2Pi
= 0.131
α = 0.403
. = 1.719
β= 0.040
= 17.298). The maxim uptake rate of brain (9.1% ± 1.0%) was reaches at lh
while at 24h
the target/noise ratio was higher. Critical organs liver
lung
spleen and kidney had high uptake rate [(9.881 1.43)- (16.29± 1.72)]
except liver
other organs showed quick clearance (T
1/2
<
4h). Thyroid had a low uptake. Autoradiography of the brain showed that striatum uptake was good
striatum /cerebral cortex radioactivity ratio achieved maximum at 20h. The results show that
-β-CIT has a high striatum uptake and good stability in vivo
can provide good SPECT forages
the best acquisition time of SPECT may be about 20h after i.v..
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