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Pharmacokinetic and pharmacodynamic effects of the novel benzodiazepine antagonist 2-phenylpyrazolo[4,3-c]quinolin-3(5H)-one in humans.

Authors
  • Reimann, I W
  • Jedrychowski, M
  • Schulz, R
  • Antonin, K H
  • Roth, A
  • Bieck, P R
Type
Published Article
Journal
Arzneimittel-Forschung
Publication Date
Oct 01, 1987
Volume
37
Issue
10
Pages
1174–1178
Identifiers
PMID: 2893624
Source
Medline
License
Unknown

Abstract

2-Phenylpyrazolo[4,3-c]quinolin-3(5H)-one (CGS 8216) is pharmacologically characterized as benzodiazepine antagonist with low inverse agonistic effects. Single oral doses up to 650 mg and subchronic doses up to 100 mg daily for seven days are well tolerated by young healthy volunteers. Plasma concentrations of CGS 8216 are variable, not dose-related and relatively low considering the doses administered. A high plasma concentration ratio of metabolite vs. parent compound (3:1) points to an extensive gastrointestinal first-pass metabolism. CGS 8216 influences the human electroencephalogram similar to anxiolytic and vigilance enhancing drugs in doses which do not change performance of psychometric tests. CGS 8216 antagonizes the diazepam-induced impairment of alertness.

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