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Effects of PAF and PAF antagonists on the shape of venous endothelial cellsin vitro

  • Platelets and Thrombosis
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Abstract

Three platelet-activating factor (PAF) antagonists were tested for their ability to prevent or reduce PAF-induced shape changes of large vein endothelial cellsin vitro. BN52021 had a significant protective action at concentrations of 1 μM and 0.1 μM, but at 100 μM had a damaging effect of its own. CV3988 (0.1 μM and 1 μM) and L652, 731 (20 μM) did not reduce the responses to PAF, and at higher concentrations (CV3988 10 μM and 100 μM, L652, 731 100 μM) both compounds alone caused significant changes of shape. BN52021 (0.1 μM) was also effective against leukotriene (LT) C4, at 1 μM against bradykinin and LTE4, and at 10 μM against LTD4 and the calcium ionophore A23187. BN52021 (10 μM) was ineffective against shape changes induced by histamine, prostaglandin (PG) E2 and lysophosphatidylcholine (LPC). Neither indomethacin (100 μM) nor verapamil (20 μM) altered the response to PAF.

Using electron spin resonance (ESR) spectrometry it was shown that the damaging effects of LPC and CV3988 may be due partly to their detergent properties. It is suggested that the mechanism by which PAF alters the shape of large vein endothelial cells is primarily receptor mediated.

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  1. Department of Pharmacology, School of Pharmacy, Leicester Polytechnic, LE1 9BH, Leicester, UK

    A. M. Northover

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Northover, A.M. Effects of PAF and PAF antagonists on the shape of venous endothelial cellsin vitro . Agents and Actions 28, 142–148 (1989). https://doi.org/10.1007/BF02022995

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