Synthesis of Fluorine and Iodine Analogues of Clorgyline and Selective Inhibition of Monoamine Oxidase A
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概要
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A series of fluorine and iodine analogues of clorgyline was synthesized and evaluated for inhibitory potency and selectivity toward monoamine oxidase A (MAO-A). Among them, N-[3(2,4-dichloro-6-iodophenoxy)propyl]-N-methyl-2-propynylamine (3d), N-[3-(4-chloro-2-fluorophenoxy)propyl]-N-methyl-2-propynylamine (3f) and N-[3-(2-chloro-4-fluorophenoxy)propyl]-N-methyl-2-propynylamine (3g) were found to have high inhibitory potency and selectivity toward MAO-A comparable to those of clorgyline itself. Thus, they were considered for advanced development as radiofluorinated and radioiodinated ligands that may be useful for functional MAO-A studies in the living brain with positron emission tomography and single photon emission computer tomography.
- 社団法人日本薬学会の論文
- 1991-04-25
著者
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横山 陽
Faculty of Pharmaceutical Sciences, Kyoto University
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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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田中 千秋
Osaka University of Pharmaceutical Sciences
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平田 雅彦
Osaka University of Pharmaceutical Sciences
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間賀田 泰寛
Kyoto University Hospital
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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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田中 千秋
Osaka College Of Pharmacy
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