Olodaterol (BI1744) hydrochloride is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis[2].IC50 & Target: EC50: 0.1 nM (β2-adrenoceptor)In Vitro: Olodaterol hydrochloride (0.1~10 nM; fibroblasts) interferes with FGF-induced phosphorylation of signalling cascades[2].
Olodaterol hydrochloride (0.001~10 nM; fibroblasts) attenuates growth factor-induced motility and proliferation[2].
Olodaterol hydrochloride (0.001~1000 nM; 0.5 hours; fibroblasts) increases intracellular cAMP in a concentration-dependent manner. Olodaterol hydrochloride (0~10 nM; 0.5 hours; fibroblasts) concentration-dependently inhibits the PICP increase with maximal efficacy of 70 % at 10 nM. Olodaterol hydrochloride has a subnanomolar affinity for the β2-AR (pKi=9.14) and is selective for this receptorin comparison with the β1-AR and β3-AR subtypes[2].In Vivo: Olodaterol (1 mg/kg; inhal.; 21 days) accelerats body weights recovery back to control levels (at day 21) and attenuats TGF-β-induced lung fibrosis[2].
Olodaterol (0.1~3 μg/kg; inhal.; 5 hours) induces a dose-dependent bronchoprotection.
Olodaterol (0.3 and 0.6 μg/kg; inhal.; 24 hours) induces a maximal bronchoprotection of approximately 60 % after 0.5 hours.