Radioiodinated N-(2-Aminoethyl)-2-chloro-4-iodobenzamide : A New Ligand for Monoamine Oxidase B Studies with Single Photon Emission Computed Tomography
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概要
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In developing monoamine oxidase (MAO)-B specific radioligands, N-(2-aminoethyl)-2-chloro-4-[^<125>I]iodobenzamide ([^<125>I]FIBA) was conveniently synthesized from its tributylstannyl precursor by an iododestannylation reaction using sodium [^<125>I]iodide and hydrogen peroxide with high radiochemical yield. The method should be applicable for labeling with ^<123>I, a suitable radioisotope for in vivo imaging with single photon emission computed tomography (SPECT). In vitro binding studies using mouse brain mitochondrial preparations showed that the specific binding of [^<125>I]FIBA was saturable and of high affinity. Calculated values for K_D and B_<max> were 201 nM and 9.5 pmol/mg protein, respectively. The [^<125>I]FIBA binding was effectively prevented by MAO-B specific inhibitors (l-deprenyl, Ro 16-6491,FIBA) or substrate (β-phenethylamine). However, MAO-A specific inhibitor (clorgyline) and substrate (serotonin) had no significant effect. After an intravenous injection into mice, [^<125>I]FIBA showed high brain uptake (1.64% dose/g at 15-30 min post injection) and long retention (1.11% dose/g at 120 min post injection) in the brain. Good brain-to-blood radioactivity ratios of 2.19 and 2.41 at 60 and 120 min after injection, respectively, were obtained. The in vitro binding data and in vivo characteristics suggested that [^<125>I]FIBA is potentially useful as a probe for biological studies including specific labeling of MAO-B in vivo as well as in vitro. Moreover, the ^<123>I-labeled counterpart, [^<123>I]FIBA, might be valuable for non-invasive imaging and mapping of MAO-B in the living brain with SPECT.
- 社団法人日本薬学会の論文
- 1994-04-15
著者
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横山 陽
Faculty of Pharmaceutical Sciences, Kyoto University
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横山 陽
京都大学薬学部
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間賀田 泰寛
京都大学医学部
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大桃 善朗
Osaka University of Pharmaceutical Sciences
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村上 勝彦
Osaka University of Pharmaceutical Sciences
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平田 雅彦
Faculty of Pharmaceutical Sciences Kyoto University
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間賀田 泰寛
School of Medicine Kyoto University
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田中 千秋
Osaka University of Pharmaceutical Sciences
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間賀田 泰寛
京都大学医学部放射線核医学講座
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横山 陽
京大
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田中 千秋
Osaka College Of Pharmacy
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