抗精神病药物的19F核磁共振波谱分析：大鼠脑中三氟拉嗪的首次体内药代动力学及人脑中氟奋乃静的首次体内波谱分析。

19F nuclear magnetic resonance spectroscopy of neuroleptics: the first in vivo pharmacokinetics of trifluoperazine in the rat brain and the first in vivo spectrum of fluphenazine in the human brain.

作者信息

Bartels M, Günther U, Albert K, Mann K, Schuff N, Stuckstedte H

机构信息

Department of Psychiatry, University of Tübingen, Germany.

出版信息

Biol Psychiatry. 1991 Oct 1;30(7):656-62. doi: 10.1016/0006-3223(91)90011-a.

DOI:10.1016/0006-3223(91)90011-a

PMID:1958765

Abstract

In vivo 19F nuclear magnetic resonance (19F-NMR) spectroscopy measurements of trifluorinated neuroleptics (fluphenazine--FL and trifluoperazine--TFP) were made in rat brain as well as in human brain. Animal studies were performed at 4.7 Tesla. Using rats that have been treated with FL over a period of 3 weeks, a NMR signal could be detected within 8-15 min. Following a single intravenous injection of TFP, brain levels could be monitored with a time resolution of 30 min. The first 19F-NMR examination of a patient was made at 3.0 Tesla 1 day after injection of FL decanoate (37.5 mg) in the course of which a signal could be detected within 30 min. It is expected that 19F-NMR will become an important tool in psychopharmacological research.

摘要

在大鼠脑和人脑中对三氟取代抗精神病药物（氟奋乃静——FL和三氟拉嗪——TFP）进行了体内19F核磁共振（19F-NMR）光谱测量。动物研究在4.7特斯拉的磁场强度下进行。使用经过3周FL治疗的大鼠，在8 - 15分钟内可检测到核磁共振信号。单次静脉注射TFP后，可每30分钟监测一次脑内药物水平。在注射癸酸氟奋乃静（37.5毫克）1天后，在3.0特斯拉的磁场强度下对一名患者进行了首次19F-NMR检查，在此过程中30分钟内即可检测到信号。预计19F-NMR将成为精神药理学研究中的一项重要工具。