Ebselen inhibits contractile responses of guinea-pig parenchymal lung strips

European Journal of Pharmacology
R LeursH Timmerman

Abstract

Ebselen is a new anti-inflammatory drug with a wide spectrum of pharmacological activities. Since this compound might be useful in diseases related to airway inflammation we evaluated the effects of ebselen on the contractile responses of guinea-pig parenchymal lung strip. Ebselen and its sulfur analogue RP 62373 depressed both histamine H1-receptor-mediated and KCl-induced (50 mM) contractions of guinea-pig lung strips equipotently. The responses to histamine were only affected via depression of the maximal response; treatment with 3 microM ebselen for 30 min resulted in depression to 77 +/- 5% of the control value, whereas 10 and 30 microM inhibited the contractions to 53 +/- 4 and 52 +/- 4% of the control value respectively. The responses after membrane depolarisation (50 mM KCl) were less sensitive to ebselen pretreatment; 10 microM ebselen inhibited contractions by only 20%, whereas 30 and 100 microM depressed the response by approximately 50%. These observations were evaluated in the context of the activities of ebselen already described. The effects of lipoxygenase, cyclooxygenase, protein kinase C inhibition and thiol alkylation were studied, using established agents. However, although interaction with critical thiol gr...Continue Reading

References

Feb 15, 1989·Biochemical Pharmacology·N Kühn-Velten, H Sies
May 29, 1987·Biochemical and Biophysical Research Communications·K KramerA Bast

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Citations

Oct 1, 1995·General Pharmacology·T Schewe
Mar 1, 1993·Free Radical Biology & Medicine·H Sies
Feb 20, 2003·European Journal of Pharmacology·Yan CheChun Guang Li
Jun 15, 1991·Biochemical Pharmacology·B BrüneV Ullrich

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