6-[124I]Iodo-9-pentylpurine for Imaging the Activity of the Sodium Iodide Symporter in the Brain.,Journal of Medicinal Chemistry

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6-[124I]Iodo-9-pentylpurine for Imaging the Activity of the Sodium Iodide Symporter in the Brain.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-02-06 , DOI: 10.1021/acs.jmedchem.9b02096
Toshimitsu Okamura ₁ , Satoshi Tsukamoto ₁ , Kotaro Nagatsu ₁ , Maki Okada ₁ , Katsuyuki Minegishi ₁ , Takayuki Tatsumi ₂ , Aya Sugyo ₁ , Tatsuya Kikuchi ₁ , Hidekatsu Wakizaka ₁ , Hideki Ishii ₁ , Atsushi B Tsuji ₁ , Ming-Rong Zhang ₁

Affiliation

Iodide homeostasis and thyroid hormone metabolism in the brain are potentially related to changes in the activity of the sodium iodide symporter (NIS). No radiotracers are currently available for imaging brain NIS activity. Here, we synthesized 6-[124I]iodo-9-pentylpurine that can noninvasively measure iodide efflux from the brain and showed that the efflux rate of [124I]I- in NIS knockout mice was 84% lower than that of wild-type mice. Thus, 6-[124I]iodo-9-pentylpurine would be useful for imaging brain NIS activity.

中文翻译：

用6- [124I]碘-9-戊基嘌呤成像脑中碘化钠同向转运蛋白的活性。

大脑中的碘化物稳态和甲状腺激素代谢可能与碘化钠共转运蛋白（NIS）活性的变化有关。当前没有放射性示踪剂可用于成像脑NIS活动。在这里，我们合成了6- [124I] io-9-戊基嘌呤，它可以无创地测量大脑中的碘流出，并显示[124I] I-在NIS基因敲除小鼠中的流出率比野生型小鼠低84％。。因此，6- [124I]碘-9-戊基嘌呤可用于成像脑NIS活性。

更新日期：2020-02-19

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