Synthesis and biological evaluation of [(18)F]tetrafluoroborate: a PET imaging agent for thyroid disease and reporter gene imaging of the sodium/iodide symporter.
Synthesis and biological evaluation of [(18)F]tetrafluoroborate: a PET imaging agent for thyroid disease and reporter gene imaging of the sodium/iodide symporter.
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DOI：
10.1007/s00259-010-1523-0
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发表时间：
2010-11
影响因子：
9.1
通讯作者：
Blower, Philip J.
中科院分区：
文献类型：
--
作者：
Jauregui-Osoro, Maite;Sunassee, Kavitha;Weeks, Amanda J.;Berry, David J.;Paul, Rowena L.;Cleij, Marcel;Banga, Jasvinder Paul;O'Doherty, Michael J.;Marsden, Paul K.;Clarke, Susan E. M.;Ballinger, James R.;Szanda, Istvan;Cheng, Sheue-Yann;Blower, Philip J.
人钠/碘同向转运体（hNIS）是甲状腺疾病和报告基因成像的一个公认靶点，使用γ发射体123 I-碘化物、131 I-碘化物和99 mTc-高锝酸盐。然而，没有常规可用的PET成像剂。本研究的目的是制备和评价用于hNIS PET成像的18F标记四氟硼酸盐（[18F]TFB）。[18 F]TFB是通过在热盐酸中用[18 F]氟化物进行BF 4 −的同位素交换制备的，并使用氧化铝柱进行纯化。采用高效液相色谱法、薄层色谱法和质谱法测定其在血清中的性质、纯度和稳定性。它与NIS的相互作用进行了评估，在体外使用FRTL-5大鼠甲状腺细胞，有和没有刺激的促甲状腺激素（TSH），在存在和不存在高氯酸盐。使用BALB/c小鼠进行生物分布和PET成像研究，有和没有高氯酸盐抑制。[18 F]TFB易于制备，比活度为10 GBq/mg。在FRTL-5细胞中的快速蓄积可被TSH刺激并被高氯酸盐抑制，在体内甲状腺（1 h后SUV = 72）和胃中的快速特异蓄积可被高氯酸盐抑制95%。[18F]TFB是一种易于制备的啮齿动物NIS PET显像剂，应在人体中评价hNIS PET显像。本文的在线版本（doi：10.1007/s 00259 -010-1523-0）包含补充材料，可供授权用户使用。
The human sodium/iodide symporter (hNIS) is a well-established target in thyroid disease and reporter gene imaging using gamma emitters 123I-iodide, 131I-iodide and 99mTc-pertechnetate. However, no PET imaging agent is routinely available. The aim of this study was to prepare and evaluate 18F-labelled tetrafluoroborate ([18F]TFB) for PET imaging of hNIS. [18F]TFB was prepared by isotopic exchange of BF4− with [18F]fluoride in hot hydrochloric acid and purified using an alumina column. Its identity, purity and stability in serum were determined by HPLC, thin-layer chromatography (TLC) and mass spectrometry. Its interaction with NIS was assessed in vitro using FRTL-5 rat thyroid cells, with and without stimulation by thyroid-stimulating hormone (TSH), in the presence and absence of perchlorate. Biodistribution and PET imaging studies were performed using BALB/c mice, with and without perchlorate inhibition. [18F]TFB was readily prepared with specific activity of 10 GBq/mg. It showed rapid accumulation in FRTL-5 cells that was stimulated by TSH and inhibited by perchlorate, and rapid specific accumulation in vivo in thyroid (SUV = 72 after 1 h) and stomach that was inhibited 95% by perchlorate. [18F]TFB is an easily prepared PET imaging agent for rodent NIS and should be evaluated for hNIS PET imaging in humans. The online version of this article (doi:10.1007/s00259-010-1523-0) contains supplementary material, which is available to authorized users.
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影响因子：
5.8
作者：
FREY, P;TOWNSEND, D;DONATH, A
通讯作者：
DONATH, A
DOI：
10.1006/bbrc.1999.0468
发表时间：
1999-04-13
影响因子：
3.1
作者：
Jeker, LT;Hejazi, M;Caturegli, P
通讯作者：
Caturegli, P
影响因子：
3.2
作者：
Jones, PA;Pendlington, RU;Barratt, MD
通讯作者：
Barratt, MD
影响因子：
9.3
作者：
Hobbs, Robert F.;Wahl, Richard L.;Sgouros, George
通讯作者：
Sgouros, George
影响因子：
3.1
作者：
Chen, Libo;Altman, Annette;Haberkorn, Uwe
通讯作者：
Haberkorn, Uwe