| Japanese |
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| Title | Paroxetineの肺機能測定放射性薬剤としての可能性の検討 |
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| Subtitle | ≪原著≫ |
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| Authors | 橋本謙二*, 五郎丸毅* |
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| Organization | *福山大学薬学部放射性薬品化学研究室 |
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| Journal | 核医学 |
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| Volume | 26 |
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| Number | 7 |
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| Page | 879-885 |
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| Year/Month | 1989/7 |
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| Article | 原著 |
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| Publisher | 日本核医学会 |
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| Abstract | 「要旨」強力なセロトニン再吸収阻害作用を有する非三環系抗うつ薬であるparoxetineの3H標識体の肺における放射性薬剤としでの可能性を評価した. 3H-paroxetineをマウスに静脈内投与し, 経時的に各臓器における放射能分布を測定した結果, 肺に非常に高い放射能の集積が見られた. しかしながら, 肺における放射能分布はキャリアであるparoxetineあるいは他のモノアミン再吸収阻害薬の投与によって減少しなかった. さらに, 3H-paroxetineのマウス肺におけるインビトロ結合飽和実験の結果より, 肺にも特異的結合部位が高密度に存在することが判った. また, トレーサ投与1時間後の肺における放射性物質をTLCおよびHPLCで分析した結果, 未変化体であることが判った. 以上の結果より, 3H-paroxetineはセロトニンの代謝臓器としての肺の機能検査に応用できる放射性薬剤になる可能性があると思われる. |
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| Practice | 臨床医学：一般 |
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| Keywords | Paroxetine, In vivo binding, Serotonin uptake, Lung, Positron emission tomography. |
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| English |
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| Title | Evaluation of 3H-Paroxetine as a Radiopharmaceutical for Lung Function |
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| Subtitle | - Original Articles - |
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| Authors | Kenji HASHIMOTO, Tsuyoshi GOROMARU |
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| Authors(kana) | |
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| Organization | Department of Radiopharmaceutical Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences, University of Fukuyama |
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| Journal | The Japanese Journal of nuclear medicine |
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| Volume | 26 |
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| Number | 7 |
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| Page | 879-885 |
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| Year/Month | 1989/7 |
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| Article | Original article |
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| Publisher | THE JAPANESE SOCIETY OF NUCLEAR MEDICINE |
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| Abstract | [Summary] The potential of 3H-paroxetine as a radiotracer for in vivo study of the function in mouse lung was examined. The high accumulation of radioactivity in the mouse lung was observed after intravenous administration of 3H-paroxetine. However, the distributions of radioactivity in the mouse lung were not significantly decreased by treatment with paroxetine or other monoamine uptake inhibitors (6-nitroquipazine, desipramine and GBR 12909). It was found that the radioactivity in the mouse lung at 1 hr after intravenous administration of 3H-paroxetine was due to unmetabolized 3H-paroxetine from TLC and HPLC analyses. Furthermore, 3H-paroxetine exhibits both saturable and high affinity binding sites in mouse lung with a maximal number of binding sites (Bmax) of 303 fmoles/mg protein and a dissociation constant (Kd) of 92.2 pM. These results suggest that 3H-paroxetine would be a suitable radiopharmaceutical for in vivo study of the function of lung as a metabolic organ of serotonin. |
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| Practice | Clinical medicine |
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| Keywords | Paroxetine, In vivo binding, Serotonin uptake, Lung, Positron emission tomography. |
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