PMID: 9442478Jan 27, 1998Paper

Effects of apafant on PAF-induced downregulation of beta-adrenoceptors in guinea pigs

Methods and Findings in Experimental and Clinical Pharmacology
Y SugimotoC Kamei

Abstract

We examined the effects of platelet-activating factor (PAF) on beta-adrenoceptors and the functional response to isoproterenol in guinea pig parenchymal strips. PAF caused a reduction in the relaxation of guinea pig lung parenchymal strips induced by the beta-adrenoceptor agonist, isoproterenol. In addition, PAF decreased the density of beta-adrenoceptors in guinea pig lung without any change in the affinity. Apafant, a potent PAF antagonist, inhibited the above changes, indicating that it inhibited the downregulation of beta-adrenoceptors. These findings suggest that apafant may be effective in nonspecific airway hyperreactivity in asthma.

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