| Japanese |
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| Title | 血中遊離型リガンド濃度の迅速測定およびベンゾジアゼピンレセプター活性の定量解析に関する研究 |
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| Subtitle | 原著 |
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| Authors | 橋本謙二*, 井上修**, 伊藤高司***, 五郎丸毅*, 山崎統四郎** |
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| Authors(kana) | |
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| Organization | *福山大学薬学部放射性薬品化学研究室, **放射線医学総合研究所臨床研究部, ***日本医科大学数学教室 |
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| Journal | 核医学 |
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| Volume | 25 |
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| Number | 11 |
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| Page | 1235-1243 |
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| Year/Month | 1988/11 |
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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」 脳内のベンゾジアゼピンレセプターの結合能(BP=Bmax/Kd)をインビボで定量解析することを目的として, 入力関数である血中の遊離型リガンド濃度を迅速に測定する方法を開発した. 3H-Ro 15-1788をマウスに静注し, 経時的に採血して代謝を検討した結果, 未変化体のRo 15-1788はクロロホルムで容易に抽出されることが判明した. 一方, 代謝物は全くクロロホルムに抽出されず, 溶媒抽出法により迅速簡便に血中のリガンド濃度を算出することができた. また, 血漿蛋白結合率は限外濾過法によって求めた. コントロールおよび強制水泳(16℃, 5分間)を負荷したマウスに3H-Ro 15-1788を静注し, 大脳皮質, 小脳および橋-延髄の放射能を経時的に測定し, 上記の方法で血中の遊離型リガンド濃度の経時変化を求めた. これらの測定値を簡単なモデルで解析してベンゾジアゼピンレセプターの結合能を算出した結果, 強制水泳によリレセプター活性(BP)が低下していることが明らかになった. 今回開発した方法は11C-Ro 15-1788とPETによる臨床データの定量解析に有用であることが判明した. |
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| Practice | 臨床医学：一般 |
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| Keywords | Ro 15-1788, Benzodiazepine receptor, Positron emission tomography, Forced-swimming, Kinetic model |
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| English |
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| Title | Study on Measurement of Free Ligand Concentration in Blood and Quantitative Analysis of Brain Benzodiazepine Receptor |
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| Authors | Kenji HASHIMOTO*, Osamu INOUE**, Takashi ITOH***, Tsuyoshi GOROMARU*, Toshiro YAMASAKI** |
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| Authors(kana) | |
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| Organization | *Department of Radiopharmaceutical Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences, University of Fukuyama, **Division of Clinical Research, National Institute of Radiological Sciences, ***Devision of Mathematics, Nippon Medical School |
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| Journal | The Japanese Journal of nuclear medicine |
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| Volume | 25 |
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| Number | 11 |
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| Page | 1235-1243 |
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| Year/Month | 1988/11 |
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| Article | Original article |
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| Publisher | THE JAPANESE SOCIETY OF NUCLEAR MEDICINE |
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| Abstract | [Summary] We developed the method to determine rapidly the free ligand concentration in the blood as an input function for the purpose of quantitative analysis of binding potential (Bmax/Kd) of brain benzodiazepine receptor in vivo. It was found that the unmetabolized radioligand in the blood after intravenous administration of 3H-Ro 15-1788 could be extracted by chloroform, whereas the radioactive metabolites could not be extracted. And the plasma protein binding of 3H-Ro 15-1788 was determined using an ultrafiltration method. The biodistribution of 3H-Ro 15-1788 in the cerebral cortex, cerebellum and pons-medulla after intravenous administration of the radiotracer in the control and forced-swimmed mice was examined. And the time course of the free ligand concentration in the blood was determined as described above. Further, the binding potential of benzodiazepine receptor in the mouse brain was analyzed using a simple mathematical model. It was suggested that the binding potential of benzodiazepine receptor in the mouse brain was significantly decreased by forced-swimming. In conclusion, it was found that these methods would be useful for quantitative analysis of clinical data in the human brain using 11C-Ro 15-1788 and positron emission tomography(PET). |
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| Practice | Clinical medicine |
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| Keywords | Ro 15-1788, Benzodiazepine receptor, Positron emission tomography, Forced-swimming, Kinetic model |
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