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2'-脱氧-2'-[18F]氟-5-溴-1-β-D-阿拉伯呋喃糖基尿嘧啶（[18F]-FBAU）和2'-脱氧-2'-[18F]氟-5-氯-1-β-D-阿拉伯呋喃糖基尿嘧啶（[18F]-FCAU）的合成及其作为基因表达标志物的生物学评价。

Synthesis of 2'-deoxy-2'-[18F]fluoro-5-bromo-1-beta-D-arabinofuranosyluracil ([18F]-FBAU) and 2'-deoxy-2'-[18F]fluoro-5-chloro-1-beta-D-arabinofuranosyl-uracil ([18F]-FCAU), and their biological evaluation as markers for gene expression.

作者信息

Alauddin Mian M, Shahinian Antranic, Park Ryan, Tohme Michel, Fissekis John D, Conti Peter S

机构信息

Department of Radiology, PET Imaging Science Center, University of Southern California, 2250 Alcazar Street, Suite 135V, Los Angeles, CA 90033, USA.

出版信息

Nucl Med Biol. 2004 May;31(4):399-405. doi: 10.1016/j.nucmedbio.2003.12.008.

DOI:10.1016/j.nucmedbio.2003.12.008
PMID:15093809
Abstract

[(18)F]-FBAU and [(18)F]-FCAU have been synthesized and evaluated in vivo as markers for HSV1-tk gene expression. At 2 hours, uptake of [(18)F]-FBAU and [(18)F]-FCAU in HSV1-tk-positive tumors was 7.9-fold and 6.0-fold higher than the control tumors, respectively. Micro-PET images also showed very high uptake in HSV-tk tumors. Compared to [(14)C]-FMAU, total uptake of [(18)F]-FBAU and [(18)F]-FCAU was similar in tk-positive cells, but the uptake ratio (tk+/wild) was higher. [(18)F]-FBAU and [(18)F]-FCAU appear to be potential PET imaging agents for gene expression.

摘要

已合成了[(18)F]-FBAU和[(18)F]-FCAU，并在体内作为单纯疱疹病毒1型胸苷激酶（HSV1-tk）基因表达的标志物进行了评估。在2小时时，[(18)F]-FBAU和[(18)F]-FCAU在HSV1-tk阳性肿瘤中的摄取分别比对照肿瘤高7.9倍和6.0倍。微型正电子发射断层扫描（Micro-PET）图像也显示HSV-tk肿瘤中有非常高的摄取。与[(14)C]-FMAU相比，[(18)F]-FBAU和[(18)F]-FCAU在tk阳性细胞中的总摄取相似，但摄取率（tk+/野生型）更高。[(18)F]-FBAU和[(18)F]-FCAU似乎是用于基因表达的潜在正电子发射断层扫描（PET）成像剂。

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