Y. Sugimoto et al., EFFECTS OF APAFANT ON PAF-INDUCED DOWN-REGULATION OF BETA-ADRENOCEPTORS IN GUINEA-PIGS, Methods and findings in experimental and clinical pharmacology, 19(8), 1997, pp. 547-552
We examined the effects of platelet-activating factor (PAF) on beta-ad
renoceptors and the functional response to isoproterenol in guinea pig
parenchymal strips. PAF caused a reduction in the relaxation of guine
a pig lung parenchymal strips induced by the beta-adrenoceptor agonist
, isoproterenol. In addition, PAF decreased the density of beta-adreno
ceptors in guinea pig lung without any change in the affinity. Apafant
, a potent PAF antagonist, inhibited the above changes, indicating tha
t it inhibited the downregulation of beta-adrenoceptors. These finding
s suggest that apafant may be effective in nonspecific airway hyperrea
ctivity in asthma.