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Basis of 5-[14C]methly-4'-thio-2'-deoxyuridine as a potential 11C-labeled cell proliferation marker:in vitro cell uptake and in vivo distribution in tumor-bearing mice.

https://repo.qst.go.jp/records/61840
https://repo.qst.go.jp/records/61840
331fce98-09b6-4f29-9a9a-baa399b71de8
Item type 会議発表用資料 / Presentation(1)
公開日 2006-10-10
タイトル
タイトル Basis of 5-[14C]methly-4'-thio-2'-deoxyuridine as a potential 11C-labeled cell proliferation marker:in vitro cell uptake and in vivo distribution in tumor-bearing mice.
言語
言語 eng
資源タイプ
資源タイプ識別子 http://purl.org/coar/resource_type/c_c94f
資源タイプ conference object
アクセス権
アクセス権 metadata only access
アクセス権URI http://purl.org/coar/access_right/c_14cb
著者 Toyohara, Jun

× Toyohara, Jun

WEKO 612061

Toyohara, Jun

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Kumata, Katsushi

× Kumata, Katsushi

WEKO 612062

Kumata, Katsushi

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Nakao, Ryuji

× Nakao, Ryuji

WEKO 612063

Nakao, Ryuji

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Kikuchi, Tatsuya

× Kikuchi, Tatsuya

WEKO 612064

Kikuchi, Tatsuya

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Fukushi, Kiyoshi

× Fukushi, Kiyoshi

WEKO 612065

Fukushi, Kiyoshi

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Suzuki, Kazutoshi

× Suzuki, Kazutoshi

WEKO 612066

Suzuki, Kazutoshi

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Irie, Toshiaki

× Irie, Toshiaki

WEKO 612067

Irie, Toshiaki

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豊原 潤

× 豊原 潤

WEKO 612068

en 豊原 潤

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熊田 勝志

× 熊田 勝志

WEKO 612069

en 熊田 勝志

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中尾 隆士

× 中尾 隆士

WEKO 612070

en 中尾 隆士

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菊池 達矢

× 菊池 達矢

WEKO 612071

en 菊池 達矢

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福士 清

× 福士 清

WEKO 612072

en 福士 清

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鈴木 和年

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WEKO 612073

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入江 俊章

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WEKO 612074

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抄録
内容記述タイプ Abstract
内容記述 Purpose: In order to obtain a thymidine analog that might prove simpler to use for imaging DNA synthesis and stimulate more widespread use of such agents, we evaluated 5-[14C]methyl-4'-thio-2'-deoxyuridine ([14C]4'-thiothymidine) as a potential 11C-labeled proliferation marker. Methods: 5-Methyl-4'-thio-2'-deoxyuridine and labeling precursor 5-trimethylstannyl-4'-thio-2'-deoxyuridine were synthesized by adapting procedure described previously [1-2]. The rapid methylation of 5-trimethylstannyl-4'-thio-2'-deoxyuridine via a palladium mediated Stille-coupling reaction with [14C]methyl iodide was performed by adapting previously described procedure [3]. Resultant [14C]4'-thiothymidine was purified by the semi-preparative HPLC. A steady-state accumulation rate, Ki (ml medium/min/g cells), was calculated from the slope of the accumulation versus time plot of in vitro C6 glioma tracer uptake. The in vivo potential of [14C]4'-thiothymidine was evaluated by distribution study of EMT-6 mammary carcinoma-bearing mice. Gemcitabine, a potent inhibitor of DNA synthesis, was used to modulate cell proliferation [4]. Results: All the compounds were characterized by 1H NMR spectroscopy and mass spectrometry. The [14C]4'-thiothymidine was obtained in 31-41% radiochemical yield (calculated from [14C]methyl iodide) at 130oC, 5 min reaction in DMF. The radiochemical purity of [14C]4'-thiothymidine was >99% and the specific activity was 2.04 GBq/mmol (according to the specific activity of [14C]methyl iodide). The accumulation of [14C]4'-thiothymidine was linear over 60 min in C6 glioma, and net accumulation rate, Ki, was calculated as 0.21. In vivo distribution study showed that cumulative accumulation of radioactivity in proliferating tissues (spleen, thymus, duodenum and tumor). On the other hand, radioactivity of non-proliferating tissues (lung, liver, kidney and muscle) was rapidly cleared in parallel with the clearance of blood radioactivity. The tumor uptake of [14C]4'-thiothymidine was high (8.8 1.2%ID/g at 60 min) and selective (Tumor to blood ratio: 12.2 5.9 at 60 min). Gemicitabine pretreatment significantly reduced the tumor uptake of [14C]4'-thiothymidine (Control:10.0 1.3 %ID/g; 0.5 mg/kg 30 min: 6.1 1.4%ID/g; 40 mg/kg 3 h: 3.2 1.5%ID/g). Conclusion: The labeling procedure was rapid and found to be suitable for 11C-labeling. Positron-labeled 5-methyl-4'-thio-2'-deoxyuridine should be useful for imaging DNA synthesis by PET. References: [1] Secrist JA III et al. J Med Chem 34:2361-66, 1991; [2] Toyohara J et al. J Nucl Med 43:1218-26, 2002; [3] Samuelsson1 L, Långström B. J Label Compd Radiopharm 46:263-72, 2003; [4] Borbath I et al. Eur J Nucl Med 29:19-27, 2002.
会議概要(会議名, 開催地, 会期, 主催者等)
内容記述タイプ Other
内容記述 Annual Congress of the European Association of Nuclear Medicine
発表年月日
日付 2006-10-04
日付タイプ Issued
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