| Japanese |
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| Title | SPECTによるドーパミンD2受容体画像化, 定量化のための125I-IBZMの合成とラット脳内動態 |
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| Subtitle | 技術報告 |
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| Authors | 松村要*, 外山宏**, 中島弘道*, 市瀬正則***, 倉見美規****, 中川毅*, 前田寿登**, 竹内昭**, 古賀佑彦** |
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| Authors(kana) | |
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| Organization | *三重大学医学部放射線医学教室, **藤田保健衛生大学放射線医学教室, ***Department of Nuclear Medicine, Mount Sinai Hospital, University of Toronto, ****日本メジフィジックス株式会社中央研究所 |
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| Journal | 核医学 |
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| Volume | 31 |
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| Number | 5 |
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| Page | 513-519 |
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| Year/Month | 1994/5 |
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| Article | 報告 |
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| Publisher | 日本核医学会 |
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| Abstract | 「要旨」123I-IBZMはドーパミンD2受容体画像化のために開発されたSPECT用製剤であり, すでにその臨床応用が試みられている. 本剤によるドーパミンD2受容体定量法の開発を目的とした基礎的検討のために125I-IBZMを合成し, ラット脳内での分布, 集積率の経時的変化等について検討した. 合成時の酸化剤としてクロラミン-Tを用い, 放射化学的収率は80〜90%であり, 放射化学的純度は81日後にても94.7%と良好であった. ラット脳への平均集積率(%dose/g)は静注60分後にて, 線条体1.72, 大脳皮質0.75, 小脳0.43であった. ハロペリドール静注による結合阻害試験にて125I-IBZM静注60分後の線条体への集積は非投与群の40.9%に減少し, 線条体ドーパミンD2受容体への特異的結合を示した. 線条体と小脳の集積比は時間とともに増加が見られ, 123I-IBZMによるSPECTでのヒト脳ドーパミンD2受容体の定量化に線条体/小脳比を用いる際にはこの点を考慮する必要があると考える. |
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| Practice | 臨床医学：一般 |
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| Keywords | 125I-(S)-(-)-3-iodo-2-hydroxy-6-methoxy-N[(1-ethyl-2-pyrrolidinyl)methyl]-benzamide (125I-IBZM), Single photon emission computed tomography (SPECT), Dopamine D2 receptor, In vivo biodistribution. |
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| English |
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| Title | In vivo Characteristics of IBZM in Rat Brains : An Agent for Quantitative SPECT Imaging of Dopamine D2 Receptors. Preparation of 125I-IBZM and Its Biodistribution and Kinetic Properties |
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| Authors | Kaname MATSUMURA*, Hiroshi TOYAMA**, Hiromichi NAKASHIMA*, Masanori ICHISE***, Miki KURAMI****, Tsuyoshi NAKAGAWA*, Hisato MAEDA**, Akira TAKEUCHI**, Sukehiko KOGA** |
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| Authors(kana) | |
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| Organization | *Department of Radiology, Mie University School of Medicine, **Department of Radiology, Fujita Health University School of Medicine, ***Department of Nuclear Medicine, Mount Sinai Hospital, University of Toronto, ****Central Research Laboratory, Nihon Medi-Physics Co., Ltd. |
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| Journal | The Japanese Journal of nuclear medicine |
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| Volume | 31 |
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| Number | 5 |
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| Page | 513-519 |
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| Year/Month | 1994/5 |
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| Article | Report |
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| Publisher | THE JAPANESE SOCIETY OF NUCLEAR MEDICINE |
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| Abstract | [Summary] 123I-(S)-(-)-3-iodo-2-hydroxy-6-methoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]-benzamide (IBZM) is a CNS dopamine D2 receptor imaging agent for SPECT and has already been used clinically in the United States, Canada and Europe. However, methods of quantitative SPECT measurement of the D2 receptor density have not been well established. We performed in vivo biodistribution studies of 125I-IBZM in rat brains as the first step toward establishment of a basis for quantitative SPECT imaging of D2 receptors in humans. 125I-IBZM was prepared by the chloramine-T method. Radiochemical yields were 80 to 90% and radiochemical purity was 94.7% on day 81 after labeling. At 10, 30, 60 and 120 min after injection of the radiopharmaceutical, the percent uptakes (% dose/g) in the rat striatum were 2.9, 1.9, 1.7 and 1.0, respectively. These kinetic data were considered suitable for SPECT imagings. Pretreatment with haloperidol (1 mg/kg) blocked specific striatal uptake and there was a significant reduction in the uptake to 40.9% of the unblocked uptake at 60 min after injection (p=0.006). The regional IBZM uptake ratio of striatum-to-cerebellum increased steadily from 1.7 at 10 min to 5.7 at 120 min. This suggests that SPECT imaging must be done during fixed time after tracer injection for the semiquantitative ratio to be meaningful. |
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| Practice | Clinical medicine |
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| Keywords | 125I-(S)-(-)-3-iodo-2-hydroxy-6-methoxy-N[(1-ethyl-2-pyrrolidinyl)methyl]-benzamide (125I-IBZM), Single photon emission computed tomography (SPECT), Dopamine D2 receptor, In vivo biodistribution. |
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