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Olodaterol

CAS No. : 868049-49-4

MCE 站：Olodaterol

产品活性：Olodaterol (BI1744) 是一种选择性、长效的 β₂-adrenoceptor (β₂-AR) 激动剂(EC₅₀=0.1 nM；pK_i= 9.14 for human β₂-adrenoceptor)。 Olodaterol 可用于慢性阻塞性肺疾病 (COPD) 和肺纤维化。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Adrenergic Receptor

In Vitro: Olodaterol (0.001~10 nM; fibroblasts) attenuates growth factor-induced motility ａnd proliferation.
Olodaterol (0.1~10 nM; fibroblasts) interferes with FGF-induced phosphorylation of signalling cascades.
Olodaterol (0.001~1000 nM; 30 minutes; fibroblasts) increases intracellular cAMP in a concentration-dependent manner. Olodaterol (0~10 nM; 30 minutes; fibroblasts) concentration-dependently inhibits the PICP increase with maximal efficacy of 70 % at 10 nM. Olodaterol has a subnanomolar affinity for the β₂-AR (pK_i=9.14) ａnd is selective for this receptorin comparison with the β₁-AR ａnd β₃-AR subtypes.

In Vivo: Olodaterol (1 mg/kg; inhal.; 21 days) accelerats body weight recovery back to control levels (at day 21) ａnd attenuats TGF-β-induced lung fibrosis.
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.

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