Ketotifen prevents terbutaline-induced down-regulation of beta-adrenoceptors in guinea pig lung.
We examined the effect of ketotifen on the down-regulation of beta-adrenoceptors in guinea pig lung chronically treated with terbutaline. There was a significant decrease in the density of beta-adrenoceptors following chronic administration of terbutaline. Ketotifen prevented the decrease in beta-adrenoceptor density induced by terbutaline in a dose-dependent fashion; ketotifen alone, also increased the density of beta-adrenoceptors. However, neither ketotifen nor terbutaline significantly changed the KD values in either group. These findings suggest that ketotifen might be valuable when beta-agonists are administered for long term treatment in asthmatic patients.
D000318:Adrenergic beta-Agonists / Q000494:pharmacology*; D000818:Animals; D001249:Asthma / Q000517:prevention & control; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D006168:Guinea Pigs; D007665:Ketotifen / Q000494:pharmacology* / Q000627:therapeutic use; D007700:Kinetics; D008168:Lung / Q000187:drug effects* / Q000378:metabolism; D008297:Male; D011943:Receptors, Adrenergic, beta / Q000187:drug effects*; D013726:Terbutaline / Q000494:pharmacology*
D000318:Adrenergic beta-Agonists; D011943:Receptors, Adrenergic, beta; D013726:Terbutaline; D007665:Ketotifen