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A Strategy for Increasing the Brain Uptake of a Radioligand in Animals: Use of a Drug that Inhibits Plasma Protein Binding
https://repo.qst.go.jp/records/44305
https://repo.qst.go.jp/records/443054ad65a4e-1298-4a2d-b626-2c6dfa47a282
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2006-06-21 | |||||
| タイトル | ||||||
| タイトル | A Strategy for Increasing the Brain Uptake of a Radioligand in Animals: Use of a Drug that Inhibits Plasma Protein Binding | |||||
| 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 |
Haradahira, Terushi
× Haradahira, Terushi× Zhang, Ming-Rong× Maeda, Jun× Okauchi, Takashi× Kawabe, Koichi× Kida, Takayo× Suzuki, Kazutoshi× Suhara, Tetsuya× 原田平 輝志× 張 明栄× 前田 純× 岡内 隆× 鈴木 和年× 須原 哲也 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | A positron-emitter labeled radioligand for the glycine-binding site of the N-methyl-D-aspartate(NMDA) receptor, [11C]L-703,717, was examined for its abillity to penetrate the brain in animals by simultaneous use with drugs having high-affinity separate binding sites on human serum albumin.[11C]L-703,717 has poor blood-brain barrier(BBB) permeability because it binds tightly to plasma proteins. C0^injection of warfarin (50-200 mg/kg), a drug that binds to albumin and resembles L-703,717 in structure, dose-dependlently enhanced the penetration by [11C]L-703,717 in mice, resulting in a five-fold increase in the brain radioactivity at 1 min after the injection. Drugs structurally unrelated to L703,717, salicylate, phenol red, and These results suggest that the simultaneous use of a drug that inhibits the binding of a radioligand to plasma proteins is a useful way to overcome the poor BBB permeability of the radioligand triggered by its tight binding to plasma proteins. In brain distribution studies in rodents, it was found that, after the increase in brain uptake with warfarin, much of the glycine site antagonist acumulates in the cerebellum but its pharmacological specifficty did not match the glycine site of NMDA receptors. NUCL MED BIOL 27;4:357-360,2000. 2000 Elsevier Science Inc. All right reserved. | |||||
| 書誌情報 |
Nuclear Medicine and Biology 巻 27, p. 357-360, 発行日 2000 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0969-8051 | |||||
