Synthesis and Characterization of ^<11>C-Labeled Fluoroclorgyline : A Monoamine Oxidase A Specific Inhibitor for Positron Emission Tomography

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概要

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• A new radioligand for monoamine oxidase type A (MAO-A), [^<11>C]fluoroclorgyline, was synthesized from its desmethyl precursor by N-methylation reaction using [^<11>C]methyl iodide with a radiochemical yield of 75-85%. The radiochemical purity of the product was more than 99% and the specific radioactivity was 7.4-18.5 GBq/μmol. The in vivo tissue distribution studies of [^<11>C]fluoroclorgyline in mice demonstrated its high initial uptake and prolonged retention in the brain, comparable to those of [^<11>C]clorgyline. A selective interaction with MAO-A in the accumulation of [^<11>C]fluoroclorgyline was confirmed by a competition experiment performed with the MAO-A specific inhibitor, clorgyline, and MAO-B specific inhibitor, l-deprenyl. These very desirable characteristics of [^<11>] fluoroclorgyline suggested that its ^<18>F labeled counterpart, [^<18>F]fluoroclorgyline, would have great potential as a longer-lived alternative to ^<11>C labeled clorgyline for in vivo studies of MAO-A in the human brain with positron emission tomography (PET).

• 社団法人日本薬学会の論文
• 1993-11-15

著者

• 横山 陽

  Faculty of Pharmaceutical Sciences, Kyoto University

• 横山 陽

  京都大学薬学部

• 間賀田 泰寛

  京都大学医学部

• 大桃 善朗

  Osaka University of Pharmaceutical Sciences

• 村上 勝彦

  Osaka University of Pharmaceutical Sciences

• 平田 雅彦

  Faculty of Pharmaceutical Sciences Kyoto University

• 間賀田 泰寛

  School of Medicine Kyoto University

• 田中 千秋

  Osaka University of Pharmaceutical Sciences

• 間賀田 泰寛

  京都大学医学部放射線核医学講座

• 横山 陽

  京大

• 田中 千秋

  Osaka College Of Pharmacy

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