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Ligand metabolites in plasma during PET‐studies with the11C‐labelled dopamine antagonists, raclopride, SCH 23390 and N‐methylspiroperidol

机译:使用 11C 标记的多巴胺拮抗剂、raclopride、SCH 23390 和 N-甲基螺哌啶醇进行 PET 研究期间血浆中的配体代谢物

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AbstractThe11C‐labelled radioligands raclopride, SCH 23390 and N‐methyl‐spiroperidol are well established for examination of central dopamine receptors by positron emission tomography (PET).Thin layer chromatography was used to examine the composition of radioactivity in plasma after intravenous injection of any of these three ligands into human subjects. For all three ligands there was a considerable metabolism during the time of a PET‐experiment but to a different degree. Forty‐two minutes after injection (11C)raclopride was unchanged to 76 per cent, (11C)N‐methylspiroperidol to 57 per cent and (11C) SCH 23390 only to 13 per cent.A time curve for ligand metabolism is necessary for compartmental analysis with an arterial input function. The considerable ligand metabolism demonstrated shortly after i.v. injection motivates further the identification of main metabolites to evaluate if they pass the blood‐brain barrier and bind to
机译:摘要11C标记的放射性配体raclopride、SCH 23390和N-甲基螺哌啶醇已通过正电子发射断层扫描(PET)检查中枢多巴胺受体。使用薄层色谱法检查将这三种配体中的任何一种静脉注射到人类受试者体内后血浆中的放射性组成。对于所有三种配体,在PET实验期间都有相当大的代谢,但程度不同。注射后42分钟,(11C)拉氯必利保持不变,为76%,(11C)N-甲基螺哌啶醇为57%,(11C)SCH 23390仅为13%。配体代谢的时间曲线对于具有动脉输入函数的房室分析是必要的。静脉注射后不久表现出的大量配体代谢进一步激发了主要代谢物的鉴定,以评估它们是否通过血脑屏障并结合

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