中文摘要：

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。

英文摘要：

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.