131I标记新型小分子肽VP2

doi:10.7538/tws.2016.29.01.0001

摘要/Abstract

摘要：

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

Abstract:

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

马欢;唐禹;杨远友;刘宁;廖家莉;杨吉军. ¹³¹I标记新型小分子肽VP2[J]. 同位素, 2016, 29(1): 1-5.

MA Huan;TANG Yu;YANG Yuan-you;LIU Ning;LIAO Jia-li;YANG Ji-jun. Preliminary Study of Radioiodination of VP2[J]. Journal of Isotopes, 2016, 29(1): 1-5.

参考文献

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¹³¹I标记新型小分子肽VP2

Preliminary Study of Radioiodination of VP2

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