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Ketotifen fumarate is an H1 antihistamine and mast cell stabilizer used in treatment of allergies and asthma orally and for allergic symptoms and allergic conjunctivitis in ophthalmic form. Ketotifen is also known for its effect of up-regulating the beta-2 adrenergic receptors, and can for that reason be combined with clenbuterol for treatment of especially severe asthma. Ketotifen inhibits phosphodiesterase, a chemical involved in the homeostatic feedback loop of beta-2 adrenergic activity. Castillo writes the following about ketotifen’s effect on beta-2 adrenergic receptor expression and the role of phosphodiesterase in asthma: In this study we observed that asthmatics had less methyltransferase activity and greater phosphodiesterase activity than healthy individuals. These enzymatic activities were nearer to values obtained in healthy individuals when we preincubated cells with ketotifen. The modulator effect of this drug on these two enzymes permits, on the one hand, to re-establish the beta-receptor numbers expressed on the membrane, and on the other hand, to inhibit mediator secretion provoked by antigenic stimulus. With its action on adenylate cyclase and phosphodiesterase activities, it allows cAMP intracellular accumulation and hinders the secretory process. Through its action on methyltransferase activity, it is responsible for the normalization of beta-receptor expression observed in asthmatic patients treated with ketotifen.[1] Raajimakers provides further analysis of ketotifen’s important action on beta-2 adrenergic receptors via phosphodiesterase inhibition; the mode of action was initially presumed to be through leukotriene antagonism (leukotrienes are fatty molecules involved in the immune cascade that are thought to contribute to inflammatory asthma): Adrenoceptor (sub)populations (alpha 1, beta and beta 1/beta 2 ratio) in human lung tissue were characterized by means of radioligand binding assays. Lung tissue specimens for these assays were obtained at thoracotomy from normal individuals and COLD patients. The patients were not receiving therapy known to influence adrenoceptor characteristics. In COLD patients, the number of alpha 1-adrenoceptors appeared to be markedly enhanced while the relative amount of beta 2-adrenoceptors was decreased. Furthermore, some adrenoceptors seemed to be correlated to pulmonary function both in the normal individuals and COLD patients. In-vitro modulation with disodium cromoglycate and ketotifen revealed therapeutic possibilities for these substances based on other pharmacological mechanisms than hitherto assumed.[2]


KETOTIFEN WARNING: Harmful if swallowed. Irritating to eyes, respiratory system and skin. In case of contact with eyes, rinse immediately with plenty of water. During research wear suitable protective clothing and gloves. Keep unprotected persons away. For use only by qualified researchers. Water hazardous. Research in a well ventilated area. Do not breathe dust, vapor, mist or gas. Do not ingest or inhale. Use safety glasses face protection. Disposal must be made according to official regulations. Wash hands after handling. Store in a cool dry place. Usual precautionary measures should be adhered to in handling the chemicals & peptides. NOT FOR HUMAN USE RESEARCH USE ONLY