Thiopentone and methohexitone enantiomers do not act stereoselectively on the oxidative response in human neutrophils in vitro

Wittmann, Sigrid and Daniels, S. and Ittner, Karl-Peter and Froehlich, Dieter (2004) Thiopentone and methohexitone enantiomers do not act stereoselectively on the oxidative response in human neutrophils in vitro. PHARMACOLOGY, 72 (1). pp. 12-19. ISSN 0031-7012

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Abstract

To elucidate potential stereoselective effects of single barbiturate isomers, we compared the inhibitory potency of single thiopentone enantiomers, two isomer-enriched mixtures of methohexitone and racemic mixtures of both barbiturates on the fMLP-induced neutrophil oxidative response. A suppression of the response to 50% compared to control required a 100-fold therapeutic concentration of methohexitone, while therapeutic concentrations of the thiopentone racemate led to a significant inhibition ( relative fluorescence of neutrophils 0.46 +/- 0.03 compared to fMLP controls). The racemate of thiopentone produced significantly greater inhibition than the single enantiomers. Stereoselectivity in favor of one isomer could not be shown for both barbiturates. The greater inhibition by the thiopentone racemate might suggest two separate binding sites for the enantiomers which are positively coupled. Copyright (C) 2004 S. Karger AG, Basel.

Item Type: Article
Uncontrolled Keywords: PHARMACOKINETICS; PHAGOCYTES; ACTIVATION; INFUSION; RECEPTOR; IMPAIRS; BLOOD; BURST; FMLP; fMLP; neutrophil; barbiturate; isomer; enantiomer; stereoselectivity
Subjects: 600 Technology > 610 Medical sciences Medicine
Divisions: Medicine > Lehrstuhl für Anästhesiologie
Medicine > Lehreinheit Pharmakologie
Depositing User: Dr. Gernot Deinzer
Date Deposited: 10 Aug 2021 06:06
Last Modified: 10 Aug 2021 06:06
URI: https://pred.uni-regensburg.de/id/eprint/38239

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