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Preparation and biological evaluation of 2-amino-6-[f-18]fluoro-9-(4-hydroxy-3-hydroxy-methylbutyl) purine (6-[f-18]fpcv) as a novel pet probe for imaging hsv1-tk reporter gene expression
Cai, Hancheng; Yin, Duanzhi; Zhang, Lan; Yang, Xlaofeng; Xu, Xiaoyan; Liu, Weiguo; Zheng, Xuesheng; Zhang, Hong; Wang, Jing; Xu, Yuhong
刊名Nuclear medicine and biology
2007-08-01
卷号34期号:6页码:717-725
关键词6-[f-18]fpcv Hsv1-tk Gene expression Pet
ISSN号0969-8051
DOI10.1016/j.nucmedbio.2007.06.005
通讯作者Yin, duanzhi(chcbati@yahoo.com.cn)
英文摘要Introduction: 2-amino-6-[f-18]fluoro-9-(4-hydroxy-3-hydroxy-methylbutyl) purine (6-[f-18]fpcv) was prepared via a one-step nucleophilic substitution and evaluated as a novel probe for imaging the expression of herpes simplex virus type i thymidine kinase (hsvi-tk) reporter gene. methods: log p of 6-[18f]fpcv was calculated in octanol/phosphate-buffered saline (pbs). stability studies were performed in pbs and bovine serum albumin (bsa). cell uptake was performed at various time points in wild-type cells and transduced cells. for in vivo studies, tumors were grown in nude mice by inoculation with c6 cells, wild type and tk positive. the radiotracer was intravenously injected to animals, and micro-pet imaging was performed. biodistribution of 6-[f-18]fpcv was performed on another group of animals at different time points. results: log p of 6-[f-18]fpcv was -0.517. 6-[f-18]fpcv was fairly stable in pbs and bsa at 6 h. the tracer uptake in c6-tk cells was 5.5-18.8 times higher than that in wild-type cells, the plasma half-life of 6-[f-18]fpcv was as follows: u t(1/2)=1.2 min and 1 t(1/2) = 73.7 min. the average ratio of tumor uptake between the transduced tumor and the wild-type tumor was 1.69 at 15 min. conclusion: biological evaluation showed that 6-[18f]fpcv is a potential probe for imaging hsv1 -tk gene expression. however, its in vivo defluorination may limit its application in pet imaging of gene expression. (c) 2007 elsevier inc. all rights reserved.
WOS关键词POSITRON-EMISSION-TOMOGRAPHY ; IN-VIVO ; THYMIDINE KINASE ; PYRIMIDINE NUCLEOSIDES ; RADIOTRACER ; THERAPY ; ANALOGS ; CANCER ; VITRO
WOS研究方向Radiology, Nuclear Medicine & Medical Imaging
WOS类目Radiology, Nuclear Medicine & Medical Imaging
语种英语
出版者ELSEVIER SCIENCE INC
WOS记录号WOS:000249157300016
内容类型期刊论文
URI标识http://www.corc.org.cn/handle/1471x/2380472
专题中国科学院大学
通讯作者Yin, Duanzhi
作者单位1.Chinese Acad Sci, Shanghai Inst Appl Phys, Res Ctr Radiopharmaceut, Shanghai 201800, Peoples R China
2.Zhejiang Univ, Affiliated Hosp 2, Sch Med, Inst Brain Med Sci, Hangzhou 310009, Peoples R China
3.Zhejiang Univ, Med Sch, Hangzhou 310009, Peoples R China
4.Zhejiang Calif Int NanoSyst Inst, Hangzhou 310029, Peoples R China
5.Chinese Acad Sci, Grad Sch, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714
Cai, Hancheng,Yin, Duanzhi,Zhang, Lan,et al. Preparation and biological evaluation of 2-amino-6-[f-18]fluoro-9-(4-hydroxy-3-hydroxy-methylbutyl) purine (6-[f-18]fpcv) as a novel pet probe for imaging hsv1-tk reporter gene expression[J]. Nuclear medicine and biology,2007,34(6):717-725.
APA Cai, Hancheng.,Yin, Duanzhi.,Zhang, Lan.,Yang, Xlaofeng.,Xu, Xiaoyan.,...&Wang, Yongxian.(2007).Preparation and biological evaluation of 2-amino-6-[f-18]fluoro-9-(4-hydroxy-3-hydroxy-methylbutyl) purine (6-[f-18]fpcv) as a novel pet probe for imaging hsv1-tk reporter gene expression.Nuclear medicine and biology,34(6),717-725.
MLA Cai, Hancheng,et al."Preparation and biological evaluation of 2-amino-6-[f-18]fluoro-9-(4-hydroxy-3-hydroxy-methylbutyl) purine (6-[f-18]fpcv) as a novel pet probe for imaging hsv1-tk reporter gene expression".Nuclear medicine and biology 34.6(2007):717-725.
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