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A $^{18}$F-labeled Glucose Analog: Synthesis Using a Click Labeling Method and In Vitro Evaluation
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  • A $^{18}$F-labeled Glucose Analog: Synthesis Using a Click Labeling Method and In Vitro Evaluation
  • A $^{18}$F-labeled Glucose Analog: Synthesis Using a Click Labeling Method and In Vitro Evaluation
저자명
Kim. Dong-Hyun,Choe. Yearn-Seong,Jung. Kyung-Ho,Lee. Kyung-Han,Choi. Joon-Young,Choi. Yong,Kim. Byung-Tae
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2008년|31권 5호|pp.587-593 (7 pages)
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대한약학회
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정기간행물|ENG|
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기타
이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

A $^{18}F$-labeled glucose analog, 4-[(2-[$^{18}F$]fluoroethyl)-1-($eta$-D-glucopyranosyl)]-1H-1,2,3-triazole ([$^{18}F$]1), was synthesized using a click labeling method and evaluated in vitro for its cellular transportation via glucose transporter (Glut-1) and its potential as a hexokinase substrate. The click labeling method was superior to conventional labeling method, due to a higher decay-corrected radiochemical yield (30% vs. 21%), higher specific activity ($59.9;GBq/{mu}mol$ vs. $23.5;GBq/{mu}mol$), and shorter synthesis time (75-80 min vs. 95-100 min). In vitro evaluation demonstrated that [$^{18}F$]1 does not act as a hexokinase substrate and has low and non-specific uptake by SNU-C5 cells. These results suggest that click chemistry offers a rapid and efficient radiolabeling method which does not require the protection of functional groups, although a triazole moiety at C1 of [$^{18}F$]1 is incompatible for hexokinase phosphorylation and facilitative diffusion via Glut-1.