RADIOACTIVE FLUORINE-LABELED IMAGE DIAGNOSTIC DRUG FOR MEASURING DRUG-METABOLIZING ENZYME ACTIVITY

To provide a 18F-labeled mequitazine derivative that has a high labeling rate of 18F and also has high drug stability after labeling.SOLUTION: The present invention discloses a compound represented by formula (I) (where Y- is an anion); a test drug for measuring metabolism containing the compound; a...

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Hauptverfasser:	MIZUTANI ASUKA, KAWAI KEIICHI, KOBAYASHI MASAKAZU, KITAMURA MASANORI, KUNISHIMA MUNETAKA, SUZUKI CHIE, MAGATA YASUHIRO
Format:	Patent
Sprache:	eng ; jpn
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Beschreibung
Zusammenfassung:	To provide a 18F-labeled mequitazine derivative that has a high labeling rate of 18F and also has high drug stability after labeling.SOLUTION: The present invention discloses a compound represented by formula (I) (where Y- is an anion); a test drug for measuring metabolism containing the compound; and a method for producing the compound that includes reacting a compound represented by formula: 18F-CH2-Y (where Y is a group detachable as an anion) with mequitazine. The test drug measures drug metabolism by measuring the amount of radioactive metabolite of the compound as biliary excretion.SELECTED DRAWING: None 【課題】１８Ｆの標識率が高く、加えて標識後の薬剤安定性が優れている１８Ｆ標識メキタジン誘導体の提供。【解決手段】式（Ｉ）：TIFF2022072154000015.tif4276（式中、Ｙ－は陰イオンを表す。）で示される化合物；前記化合物を含有する代謝機能を測定するための検査薬；及び式：１８Ｆ－ＣＨ２－Ｙ（式中、Ｙは陰イオンとして脱離しうる基を表す。）で示される化合物をメキタジンと反応させることを含む、前記化合物の製造方法。胆汁排泄された当該化合物の放射性代謝物の量を測定することによって薬物代謝機能を測定するための検査薬。【選択図】なし