Involvement of endothelium in relaxant action of glibenclamide on the rat mesenteric artery

European Journal of Pharmacology
Y Huang, N W Chan

Abstract

The present report describes the complex effect of glibenclamide, an antidiabetic sulfonylurea agent, on the rat isolated mesenteric artery. Although glibenclamide concentration dependently reversed the relaxant effect of pinacidil, an activator of ATP-sensitive K+ channels (the concentration for half-maximum reversal effect was 0.56 microM with endothelium and 0.17 microM without endothelium), in the artery precontracted with phenylephrine (1 microM), it relaxed phenylephrine-induced sustained contraction at higher concentrations (IC50: 4.4+/-1.1 microM with endothelium and 226.1+/-44.2 microM without endothelium). The relaxant effect of glibenclamide was partially inhibited by pretreatment of the artery with either NG-nitro-L-arginine (10-100 microM) or methylene blue (1 microM). Indomethacin (10 microM) had no effect. Moreover, glibenclamide also concentration dependently (3-500 microM) reduced the sustained contraction induced by 60 mM K+ (IC50: 99.5+/-16.1 microM). The relaxation induced by glibenclamide was not affected by various putative K+ channel blockers such as charybdotoxin (100 nM), tetraethylammonium ions (1 mM), apamin (100 nM) and 4-aminopyridine (1 mM). The results indicate an involvement of the endothelium, p...Continue Reading

References

Dec 17, 1991·European Journal of Pharmacology·J E Nielsen-Kudsk, S Thirstrup
Jan 1, 1991·British Journal of Pharmacology·K YoshitakeH Kanaide
Jan 1, 1990·Cellular Signalling·S J Ashcroft, F M Ashcroft
May 1, 1989·British Journal of Pharmacology·R E BuckinghamC Wilson
Nov 1, 1989·Trends in Pharmacological Sciences·U Quast, N S Cook

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