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http://www.ncbi.nlm.nih.gov/entrez/q...777&query_hl=6Effects of ketotifen on the responsiveness of peripheral blood lymphocyte beta-adrenergic receptors.
"The effects of ketotifen therapy on the responsiveness of lymphocyte beta-adrenergic receptors was evaluated by measuring cyclic AMP elevations caused by isoproterenol [a beta2-agonist] in cells isolated from patients treated with ketotifen for more than 1 year. Binding of 3H-dihydroalprenolol to beta-receptors was also evaluated. The isoproterenol-induced rise in cyclic AMP relative to each individual's baseline level was greater in patients on current ketotifen therapy than in other asthmatic patients or non-asthmatic subjects. Ketotifen therapy increased the apparent equilibrium dissociation constant for specific 3H-dihydroalprenolol binding to the receptors. Receptor numbers in symptomatic asthma patients on standard drug therapy were decreased. The results indicate that long term ketotifen therapy is associated with increased responsiveness of beta-receptors to stimulation by catecholamines and that this alteration may involve changes in the receptors themselves, their membrane environment, adenylate cyclase or components of the adenylate cyclase coupling system."
http://www.ncbi.nlm.nih.gov/entrez/q...319&query_hl=2Effects of ketotifen and clenbuterol on beta-adrenergic receptor functions of lymphocytes
"Applying ketotifen and clenbuterol together the beta-adrenergic receptor function increased compared to the values obtained after application of clenbuterol alone (intraindividual-control) as well as vs. the group of healthies (control). Data presented support the view that therapeutic doses of selective beta 2-agonists do not lead to damage of the beta-adrenoceptor function. The improvement of receptor function after parallel administration of clenbuterol and ketotifen may be a consequence of the participation of ketotifen in the control of beta-adrenergic receptor system."
http://www.ncbi.nlm.nih.gov/entrez/q...180&query_hl=6Effects... of ketotifen on beta 2 adrenergic receptor regulation in intact human lymphocytes
"KET alone also induced an up-regulation of cell surface beta adrenergic receptors."
http://www.ncbi.nlm.nih.gov/entrez/q...002&query_hl=6[Bronchial adrenergic receptors and asthma. Tachyphylaxis and its prevention]
(Tachyphylaxis is rapidly diminishing response to successive doses of a drug, rendering it less effective)
"The majority of the clinical studies in healthy volunteers have shown that chronic inhalation or oral intake of sympathomimetics causes tachyphylaxis of the bronchial beta adrenergic receptors... Several well controlled studies have however shown that chronic administration of sympathomimetics results in a significantly decreased sensitivity of the bronchial beta adrenergic receptor... Corticosteroids, given orally or parenterally, restore the sensitivity of the beta adrenergic receptors. In a double blind, placebo controlled study in healthy subjects we have observed that ketotifen prevents the development of a tachyphylaxis of the bronchial beta adrenergic receptor during prolonged treatment with inhaled sympathomimetics."