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p-(18)FFSTC的合成和初步动物学评价 被引量：1

Synthesis and Preliminary Biological Evaluation of p-[^(18)F]FSTC
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摘要 碳酸酐酶Ⅸ(CA Ⅸ)是一个非常有前景的肿瘤乏氧显像的靶点,而一些磺胺类化合物和CAⅨ有特异性结合。为研发一种用于CA Ⅸ检测的特异性正电子发射断层显像(PET)探针,应用点击化学(clickchem-istry)方法快速高效地合成了对CA Ⅸ有特异性结合的含氟磺胺类化合物1-(2-[18F]氟乙基)-N-(4-磺酰胺基苯基)-1H-1,2,3-三氮唑-4-酰胺(p-[18F]FSTC),合成时间约60min,标记率为90%,标记物经高效液相分离后放化纯度大于98%。p-[18F]FSTC在体内外稳定,正常小鼠体内分布结果显示,在血液中的清除较慢,脾、肺、肾和胃中的摄取较高。本工作为进一步研究18F标记的磺胺类化合物作为一种肿瘤乏氧显像PET探针提供了实验依据。 Carbonic anhydraseⅨ（CA Ⅸ） is a promising target for tumor hypoxia imaging,and some sulfamide compounds can specifically bind to human CA Ⅸ.In order to explore a novel positron emission tomography（PET） probe for detecting CA Ⅸ,the 1-（2-[18F]fluoroethyl） -N-（4-sulfamoylphenyl） -1H-1,2,3-triazole-4-carboxamide（p-[18 F]FSTC） which has specific binding affinity to CA Ⅸwas radio-synthesized fast and efficiently by a＂click chemistry＂method.The labeling efficiency of p-[18F]FSTC is 90%and the total synthesis time is about 60min.The radiochemical purity of p-[18 F]FSTC is over 98%after HPLC purification.The stability of p-[18F]FSTC both in vitro and in vivois high.The biodistribution ofp-[18F]FSTC in normal mice shows that the clearance of p-[18 F]FSTC in the blood is very slow;the uptake in spleen,lung,kidney and stomach is high.These preliminary results provide some experimental basis for further study of fluorine-18labeled sulfamide as PET probes for tumor hypoxia imaging.
作者 郭飞虎 施玲丽 王妮 武明星 张勇平 杜进 张岚
机构地区 中国原子能科学研究院同位素研究所 中国科学院上海应用物理研究所放射性药物研究中心 复旦大学附属肿瘤医院核医学科PET中心 中国同位素公司
出处 《核化学与放射化学》 CAS CSCD 北大核心 2010年第4期236-242,共7页 Journal of Nuclear and Radiochemistry
基金 国家自然科学基金资助项目(30670584,20601028)
关键词 PET 肿瘤乏氧 碳酸酐酶Ⅸ(CA Ⅸ) 磺胺类化合物 点击化学 PET tumor hypoxia carbonic anhydrase Ⅸ（CA Ⅸ） sulfamide compounds click chemistry
分类号 R817.4 [医药卫生—影像医学与核医学]
作者简介 郭飞虎（1981-），男，甘肃会宁人，博士研究生，核技术及应用专业 通讯联系人：杜进，男，博士，研究员，E-mail：dujin@china—isotope．com 通讯联系人：张岚，男，博士，副研究员，E—mail：zhanglan@sinap．ac．cn
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参考文献21

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二级参考文献23

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共引文献6

同被引文献68

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核化学与放射化学
2010年 第4期

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