(131)I标记新型小分子肽VP2

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48h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。...

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Bibliographic Details
Published in:同位素 Vol. 29; no. 1; pp. 1 - 5
Main Author: 马欢 唐禹 杨远友 刘宁 廖家莉 杨吉军
Format: Journal Article
Language:Chinese
Published: 2016
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Summary: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48h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。
Bibliography:11-2566/TL
MA Huan;TANG Yu;YANG Yuan-you;LIU Ning;LIAO Jia-li;YANG Ji-jun;Key Laboratory of Radiation Physics and Technology,Ministry of Education,Institute of NuclearScience and Technology,Sichuan University; Chengdu 610064, China
The VP2 peptide specifically binding to vasoactive intestinal polypeptide receptor 1(VPAC1)receptor was radioiodinated with 131 I by bi-functional linker Nsuccinimidyl 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 Na131I.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 6hinjection,especially in thyroid.The result indicated the labeled compound had fast clearance and good stability in vivo.
131I; VP2; labeled compound; peptide; biodistribution
ISSN:1000-7512