| Literature DB >> 10619191 |
H Russ1, T Müller, D Woitalla, A Rahbar, J Hahn, W Kuhn.
Abstract
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.Entities:
Mesh:
Substances:
Year: 1999 PMID: 10619191 DOI: 10.1007/s002109900168
Source DB: PubMed Journal: Naunyn Schmiedebergs Arch Pharmacol ISSN: 0028-1298 Impact factor: 3.000