Simplified multidose preparation of iodine-123-beta-CIT: a marker for dopamine transporters.
Simplified multidose preparation of iodine-123-beta-CIT: a marker for dopamine transporters.
复制标题
碘-123-β-CIT 的简化多剂量制备：多巴胺转运蛋白的标记物。
作者：
Y. Zea‐Ponce;R. Baldwin;M. Laruelle;S. Wang;J. Neumeyer;R. Innis
未标记
碘-123-β-CIT是多巴胺和5-HT转运蛋白的SPECT放射性配体，可能用于帕金森病、精神分裂症和可卡因成瘾研究。目前，无载体添加（NCA）[123 I] beta-CIT的制备是通过在氧化剂存在下用[123 I]碘化钠对三烷基甲锡烷基前体进行碘脱锡基化，然后进行制备型HPLC来实现的。本研究的目的是开发一种更快，更简单的方法，用于常规制备这种放射性药物。
方法
通过使用C-18 Sep-Pak Light柱的固相萃取（SPE）完成标记化合物的纯化，该柱去除未反应的碘化物、反应试剂、极性副产物和三丁基甲锡烷基前体。三丁基甲锡烷基前体优选作为起始材料，而不是三甲基甲锡烷基前体，这是由于其更高的亲脂性，允许标记产物和前体更好地分离。开发了TLC方法来评估最终产品的放射化学纯度。
结果
该方法在1.5小时内以高放射化学产率（75% +/-4%）、高放射化学纯度（>或= 98%）和比活度（> 67000 Ci/mmole）产生[123 I] β-CIT。
结论
通过固相萃取获得的结果与通过HPLC方法获得的结果一致;优点是SPE方法不需要溶剂萃取、减压蒸发或HPLC纯化。
UNLABELLED
Iodine-123-beta-CIT is a SPECT radioligand for dopamine and 5-HT transporters with potential use in Parkinson's disease, schizophrenia and cocaine addiction studies. At present, preparation of no-carrier-added (NCA) [123I] beta-CIT is achieved by iododestannylation of a trialkylstannyl precursor with sodium [123I]iodide in the presence of oxidizing agent, followed by preparative HPLC. The purpose of this study was to develop a faster and simpler method for the routine preparation of this radiopharmaceutical.
METHODS
Purification of the labeled compound was accomplished by solid phase extraction (SPE) with a C-18 Sep-Pak Light cartridge, which removed unreacted iodide, reaction reagents, polar side products and tributylstannyl precursor. The tributylstannyl precursor was preferred as starting material over the trimethylstannyl precursor due to its higher lipophilicity, allowing better separation of the labeled product and precursor. A TLC method was developed to assess the radiochemical purity of the final product.
RESULTS
The method produced [123I] beta-CIT in high radiochemical yields (75% +/- 4%), with high radiochemical purity (> or = 98%) and specific activity (> 67000 Ci/mmole), in 1.5 hr. The final formulation was sterile and pyrogen free.
CONCLUSION
The results obtained by solid phase extraction are consistent with those obtained by the HPLC method; with the advantage that the SPE method does not require solvent extraction, evaporation under reduced pressure or HPLC purification.
可卡因和相关药物对非人类灵长类动物的影响。
DOI：
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发表时间：
1989
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
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作者：
Madras,BK;Fahey,MA;Bergman,J;Canfield,DR;Spealman,RD
通讯作者：
Spealman,RD