Detection of tolcapone in the cerebrospinal fluid of parkinsonian subjects

被引：42

作者：

Russ, H

Müller, T

Woitalla, D

Rahbar, A

Hahn, J

Kuhn, W

机构：

[1] Ruhr Univ Bochum, Dept Neurol, St Josef Hosp, D-44791 Bochum, Germany

[2] Univ Regensburg, Dept Neurol, D-93053 Regensburg, Germany

来源：

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY | 1999年 / 360卷 / 06期

关键词：

tolcapone; cerebrospinal fluid; Parkinson's disease;

D O I：

10.1007/s002109900168

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The cerebral availability of the peripherally and centrally acting catechol-O-methyltransferase (COMT) inhibitor tolcapone is not known in humans. Therefore, we determined the concentration of tolcapone in cerebrospinal fluid (CSF) of 12 parkinsonian subjects 1-4 h after oral application of 200 mg of the drug. The mean concentration was 56.4+/-35.5 nmol/l (mean +/- SD), This concentration was calculated to cause 75.2+/-15% (mean +/- SD) inhibition of COMT in CSF. Thus, tolcapone efficiently inhibits COMT after crossing the blood-brain barrier in humans.

引用

页码：719 / 720

页数：2

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