| Japanese |
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| Title | N-Isopropyl-p- (I-125) Iodoamphetamineのラット脳における結合部位および細胞下分布 |
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| Subtitle | 《原著》 |
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| Authors | 森厚文*, 柴和弘*, 辻志郎**, 松田博史**, 久田欣一** |
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| Organization | *金沢大学アイソトープ総合センター, **医学部核医学科 |
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| Journal | 核医学 |
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| Volume | 23 |
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| Number | 11 |
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| Page | 1585-1594 |
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| Year/Month | 1986/11 |
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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」: N-Isopropyl-Iodoamphetamine (IMP) の脳内局在機序の解明のため, ラット脳を用いて結合アッセイならびに細胞分画実験を行い, IMPの結合部位および細胞下分布について検討した. 飽和実験より125I-IMP結合の最大結合量 (Bmax) および解離定数 (Kd) はそれぞれ15.7nmol/mgタンパクおよび56μMと非常に高い値を示し, IMPはアミン受容体のみではなく, より大容量で親和性の低い細胞成分に結合していると推定された. 阻害実験では薬物による阻害特異性が認められ, IMP結合にはパラの位置にハロゲンのついたベンゼン環とアミン部の存在および両者の配置が重要と考えられた. また細胞分画実験よりシナプス膜分画の単位タンパク量当たりの取り込み率が全脳平均の約4倍と高く, 神経細胞に特有な構造であるシナプス膜にIMPに結合しやすい化学構造を有する成分が多いことが示唆された. |
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| Practice | 臨床医学：一般 |
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| Keywords | N-isopropyl-p-Iodoamphetamine, Binding assay, Subcellular distribution, Synaptic membrane, Brain. |
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| English |
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| Title | Binding Sites and Subcellular Distribution of N-Isopropyl-p- (I-125) Iodoamphetamine in the Rat Brain |
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| Subtitle | Original Articles |
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| Authors | Hirofumi MORI*, Kazuhiro SHIBA*, Shiro TSUJI**, Hiroshi MATSUDA**, Kinichi HISADA** |
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| Authors(kana) | |
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| Organization | *Radioisotope Center, **Department of Nuclear Medicine, School of Medicine, Kanazawa University |
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| Journal | The Japanese Journal of nuclear medicine |
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| Volume | 23 |
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| Number | 11 |
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| Page | 1585-1594 |
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| Year/Month | 1986/11 |
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| Article | Original article |
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| Publisher | THE JAPANESE SOCIETY OF NUCLEAR MEDICINE |
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| Abstract | [Summary] : N-Isopropyl-p- (I-123) Iodoamphetamine (IMP) is a radioactive tracer with high lipophilic properties that has turned out useful for the assessment of regional cerebral blood flow using single-photon emission computed tomography. In this study the binding sites and subcellular distribution of IMP in the rat brain were assessed in order to elucidate the mechanism for localization of IMP in the brain. Binding assays showed that specific binding of I-125-IMP (IMP binding) in crude synaptosomal fraction was saturable with an apparent dissociation constant, Kd of 56μM and an estimated maximum number of binding sites, Bmax of 15.7 nmol/mg protein. These very high density binding sites suggest that IMP binding may be associated with the high-capacity, relatively non-specific binding sites rather than any previously described amine receptor site. The pharmacological experiments demonstrated that IMP binding to crude synaptosomal fraction was inhibited by various drugs. The presence of both of the benzene ring with halogene at the para position and the N region of the amine, and the distance of these functional groups might be related closely with IMP binding. Furthermore, it was suggested that the synaptic membrane has relatively high density of binding sites for IMP, since the subcellular fraction study showed that the synaptic membrane fraction had higher specific activity (% dose/g Protein) than other fractions. |
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| Practice | Clinical medicine |
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| Keywords | N-isopropyl-p-Iodoamphetamine, Binding assay, Subcellular distribution, Synaptic membrane, Brain. |
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