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Development of Purine-Derived 18F‑Labeled Pro-drug Tracers for Imaging of MRP1 Activity with PET
https://repo.qst.go.jp/records/46984
https://repo.qst.go.jp/records/4698476d1ed26-4cd0-4365-a34e-66fa0a21dcb5
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2014-12-16 | |||||
| タイトル | ||||||
| タイトル | Development of Purine-Derived 18F‑Labeled Pro-drug Tracers for Imaging of MRP1 Activity with PET | |||||
| 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_6501 | |||||
| 資源タイプ | journal article | |||||
| 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 |
Galante, Eva
× Galante, Eva× Okamura, Toshimitsu× Sander, Kerstin× Kikuchi, Tatsuya× Okada, Maki× Zhang, Ming-Rong× Robson, Mathew× Badar, Adam× Lythgoe, Mark× Koepp, Matthias× Årstad, Erik× 岡村 敏充× 菊池 達矢× 岡田 真希× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Multidrug resistance-associated protein 1 (MRP1) is a drug efflux transporter that has been implicated in the pathology of several neurological diseases and is associated with development of multidrug resistance. To enable measurement of MRP1 function in the living brain, a series of 6-halopurines decorated with fluorinated side chains have been synthesized and evaluated as putative pro-drug tracers. The tracers were designed to undergo conjugation with glutathione within the brain and hence form the corresponding MRP1 substrate tracers in situ. 6-Bromo-7-(2- [18F]fluoroethyl)purine showed good brain uptake and rapid metabolic conversion. Dynamic PET imaging demonstrated a marked difference in brain clearance rates between wild-type and mrp1 knockout mice, suggesting that the tracer can allow noninvasive assessment of MRP1 activity in vivo. |
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| 書誌情報 |
Journal of Medicinal Chemistry 巻 57, 号 3, p. 1023-1032, 発行日 2014-02 |
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| PubMed番号 | ||||||
| 識別子タイプ | PMID | |||||
| 関連識別子 | 24456310 | |||||
