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KMID : 0370019910050000065
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Chung-Ang Journal of Pharmacal Sciences
1991 Volume.5 No. 0 p.65 ~ p.74
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Effects of CV3988 on the Endothelium-Dependent Vasodilatory Response of PAF in the Isolated Rat Thoracic Aorta
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Abstract
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The inhibition of CV3988, a PAF antagonist, on PAF-induced relaxation was examined in the intact endothelium of the isolated rat thoracic aorta.
In the intact endothelium, PAF caused vasodilation dose-dependently even without platelets.
Whereas, in the disrupted endothelium, the complete loss of relaxation of PAF was demonstrated.
In this experiment, acetylcholine, previously reported as an endothelium-dependent vascular relaxant, also showed the relaxation in the intact endothelium, but not in the damaged endothelium.
This PAF-induced relaxation and the relaxation of acetylcho-line were slightly suppressed by pretreatment with 10^-6M CV3988.
But pretreatment with 10^-5M CV3988 significantly inhibited the relaxation of both PAF and acetylcholine on the aortic preparations.
These findings suggest that the inhibitory effect of CV3988 on PAF-induced relaxation is not by the competitive receptor antagonism to PAF, but the nonspecific inhibition due to the damage of endothelium cell.
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