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Preliminary Study of Radioiodination of VP2

MA Huan;TANG Yu;YANG Yuan-you;LIU Ning;LIAO Jia-li;YANG Ji-jun   

  1. Key Laboratory of Radiation Physics and Technology, Ministry of Education,Institute of NuclearScience and Technology, Sichuan University, Chengdu 610064, China
  • Online:2016-02-20 Published:2016-03-01



  1. 四川大学 原子核科学技术研究所 辐射物理及技术教育部重点实验室,四川 成都610064


The VP2 peptide specifically binding to vasoactive intestinal polypeptide receptor 1(VPAC1) receptor was radioiodinated with 131I by bi-functional linker N-succinimidyl 5-(tributylstannyl)-3-pyridinecarboxylate (SPC), and in vitro and in vivo stability of the labeled peptide were evaluated. Mice were injected intravenously with either 1.2×106 Bq 131I-SPC-VP2 or Na 131I. Radiochemical purity and biodistribution were studied at various time points. The result showed that purified 131I-SPC-VP2 exhibited radiochemical purity of 97% at room temperature up to 48 h. The tissue uptake of 131I-SPC-VP2 was low after 6 h injection, especially in thyroid. The result indicated the labeled compound had fast clearance and good stability in vivo.

Key words: 131I, VP2, labeled compound, peptide, biodistribution


本文通过双功能偶联剂5-(三正丁基锡)-3-吡啶甲酸-N-琥珀酰亚胺酯(SPC)将131I标记到小分子融合多肽VP2上,研究了131I标记多肽VP2的体内外稳定性及在正常小鼠体内的代谢与分布。结果表明,该标记药物室温下放置48 h后放化纯度仍可达97%,其在小鼠体内可通过胃肠道快速代谢,在甲状腺的摄取较低。用间接标记法得到的131I-SPC-VP2在体内外有良好的稳定性。

关键词: 131I, VP2, 标记药物, 小分子肽, 生物分布