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A selective β2-AR agonist
Olodaterol is a selective agonist of β2-adrenergic receptors (β2-ARs; EC50s = 97.7 and 2,725 nM for human β2- and β1-ARs, respectively). In vivo, olodaterol completely reverses acetylcholine-induced bronchoconstriction without cardiovascular side effects in guinea pigs. It also exhibits dose-dependent bronchoprotection in a beagle model of acetylcholine-induced bronchoconstriction for a period of 24 hours, indicating potential for once-daily dosing. Formulations containing olodaterol have been used to treat bronchoconstriction associated with chronic obstructive pulmonary disease.
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