囊泡乙酰胆碱转运蛋白显像剂^(123)I-IBVM的制备及SPECT脑显像

Preparation of [^(123)I]-IBVM,A Vesicular Acetylcholine Transporter Imaging Agent,for SPECT Brain Imaging

目的:研究脑囊泡乙酰胆碱转运蛋白(VAChT)显像剂123I-5-(三丁基锡-3-苯基哌啶基)-2-羟基萘(123I-IBVM)的制备及其SPECT脑显像。方法:用放射性碘氧化反应法进行IBVM前体的123I标记,用半制备高效液相色谱法(HPLC)分离纯化标记产品123I-IBVM,并测定其标记率、放化纯度及光学纯度;用123I-IBVM进行正常老年人的SPECT脑显像。结果:碘氧化反应法标记IBVM前体标记方法简便,产出率大于50%,标记产品123I-IBVM的放化纯度及光学纯度均大于95%,其在正常老年人的SPECT脑显像图像清晰。结论:123I-IBVM注射液安全、有效,可用于VAChT的SPECT脑显像研究。

Objective： To prepare 1231-5- （three phenyl butyl tin -3- piperidyl） -2- hydroxy naphtha- lene （123 I-IBVM ）, a vesicular acetylcholine transporter imaging agent for SPECT brain imaging. Methods： Radioactive iodine oxidation reaction method was employed to sign IBVM precursor with 123 I. The products were isolated and purified with semi preparative high performance liquid chromatog- raphy （HPLC）, and labeling rates, radiochemieal purity and optical purity were detected. The pre- pared 123I-IBVM was used for SPECT brain imaging. Results： The labeling yield was more than 50%. The radioehemical purity and optical purity were more than 95 %. SPECT brain images showed by 123 I- IBVM were clear. Conclusion： Prepared ~23 I-IBVM is safe and effective, and can be used for SPECT brain imaging.