Platelet-mediated vascular contractions. Inhibition by flunarizine, a calcium-entry blocker

Biochemical Pharmacology
F De Clerck, J M Van Nueten

Abstract

Flunarizine, a calcium (Ca2+)-entry blocker, selective for vascular tissues, inhibits in a concn-dependent way the contraction of isolated rat caudal artery preparations induced by mediators derived from thrombin-stimulated rat platelets. This inhibition is slow in onset and is of prolonged duration. Specific measurements and pharmacological analysis show 5-hydroxytryptamine (5HT) and thromboxane A2 (TXA2) to be the main mediators involved. Comparison with exogenously added agonists shows amplification between 5HT and TXA2 at the level of the vascular smooth muscle cells. Combined treatment with ketanserin, a selective 5HT2 receptor antagonist, and suprofen, a fatty acid cyclo-oxygenase inhibitor, shows that flunarizine inhibits the 5HT-induced as well as the prostaglandin-induced components of the contraction. The compound does not affect the release of 5HT from the platelet and does not interfere with the biosynthesis of TXA2 from endogenous platelet arachidonic acid; it reduces the amounts of TXB2 and HHT and increases the production of HETE from exogenous [14C]arachidonic acid by washed rat platelets.

References

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Citations

Dec 1, 1984·Agents and Actions·F De ClerckR S Reneman
Aug 3, 1993·European Journal of Pharmacology·W A BaxP R Saxena
Apr 4, 1996·European Journal of Pharmacology·J ZwavelingP A Van Zwieten
Jan 1, 1985·General Pharmacology·F V DeFeudis
Sep 1, 1990·Digestive Diseases and Sciences·B van OoijenJ H Wilson
Aug 1, 1993·Prostaglandins, Leukotrienes, and Essential Fatty Acids·P Puig-ParelladaJ Obach
Mar 15, 1986·Biochemical Pharmacology·J R BeetensF De Clerck
Feb 18, 1992·Biochemical Pharmacology·H Vanden BosscheP A Janssen
Jan 1, 1988·Annals of the New York Academy of Sciences·J M van NuetenP M Vanhoutte
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Jun 30, 1984·Toxicology and Applied Pharmacology·D E Mais, T R Bosin
Nov 1, 1991·Stroke; a Journal of Cerebral Circulation·R JosephK M Welch
Jan 1, 1988·Acta Oto-laryngologica. Supplementum·J M Van Nueten, W J Janssens
Jan 1, 1986·Acta Pharmacologica Et Toxicologica·K E AnderssonT Ryman
Jan 1, 1985·Acta Pharmacologica Et Toxicologica·K E Andersson
Jul 1, 1985·Pharmacological Research Communications·J M Van NuetenP M Vanhoutte

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