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The influence of endothelium on the action of PGF2α, and some dihydropyridine-type calcium antagonists in porcine basilar arteries

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Summary

Vascular endothelium modulates the effect of various vasoconstricting mediators as well as the affinity of dihydropyridine-type calcium entry blockers. To further investigate this influence, vasoconstriction by PGF2α as opposed to KCl and the affinity of nitrendipine and some related 3-ester side-chain derivatives were determined in isolated porcine basilar arteries in the presence and in the absence of intact endothelium, as well as in the presence of methylene blue. Treatment with methylene blue or mechanical endothelial damage increased the contractile work of basilar arteries stimulated by PGF2α and reduced the affinity of the dihydropyridines in such precontracted vessels. Both experimental conditions resulted in nearly the same effect. In addition, the degree of intact endothelium, as determined by substance-P-induced vasodilation, significantly correlated with the corresponding efficacy of all dihydropyridines examined. In contrast, KCl-mediated contractions remained unchanged. It is suggested that the endothelium (probably due to the production and release of endothelium-derived vasorelaxing factors, such as EDRF and/or prostacyclin) may attenuate PGF2α induced transmembrane calcium influx through receptor operated calcium channels, whereas potential operated calcium channels seems to be unaffected.

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  1. G. Kojda

    Present address: Institut für Pharmakologie der Universität Düsseldorf, Moorenstr. 5, D-4000, Düsseldorf 1

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  1. Institut für Pharmakologie der Universität zu Köln, Gleueler Straße 24, 5000, Köln, Germany

    G. Kojda, W. Klaus, G. Werner &  U. Fricke

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Dedicated to Prof. Dr. rer. nat. Dr. med. Ernst Mutschler on the occasion of his 60th birthday

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Kojda, G., Klaus, W., Werner, G. et al. The influence of endothelium on the action of PGF2α, and some dihydropyridine-type calcium antagonists in porcine basilar arteries. Basic Res Cardiol 86, 254–265 (1991). https://doi.org/10.1007/BF02190605

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