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Bitolterol Mesylate
The mesylate salt of bitolterol, a diester sympathomimetic amine with bronchodilator activity. As an ester prodrug, bitolterol is hydrolyzed by esterases to its active metabolite colterol (N-t-butylarterenol). Colterol selectively binds to and activates beta-2 adrenergic receptors in bronchiolar smooth muscle, thereby causing stimulation of adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased intracellular cAMP levels cause relaxation of bronchial smooth muscle. This increases air flow and prevents bronchospasms and may eventually lead to an improvement of airway function. (NCI Thesaurus)
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