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  • Title: Effects of apafant on PAF-induced downregulation of beta-adrenoceptors in guinea pigs.
    Author: Sugimoto Y, Nakayama Y, Kishida H, Hayakawa T, Fujiwara R, Kamei C.
    Journal: Methods Find Exp Clin Pharmacol; 1997 Oct; 19(8):547-52. PubMed ID: 9442478.
    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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