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Indacaterol maleate

CAS No. : 753498-25-8

MCE 站：Indacaterol maleate

产品活性：Indacaterol (QAB149) 马来酸盐是超长效β-肾上腺素受体激动剂。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Adrenergic Receptor

In Vivo: Indacaterol (QAB149) inhibits cAMP production in Chinese hamster ovary cells stably transfected with human β2 adrenoceptors with pEC₅₀ of 8.06. Indacaterol (QAB149) inhibits electrically induced contraction on the electrically stimulated guinea pig trachea in a concentration-dependent manner with pEC₅₀ of 8.23. Indacaterol induces a concentration-dependent inotropic effect with maximal efficacy of 75% in the isolated guinea pig left atrium. Indacaterol reverses the carbachol-induced contraction in a concentration-dependent manner with IC₅₀ of 37 nM in human small airways. Indacaterol concentration dependently reverses the serotonin-induced contraction with IC₅₀ of 10.5 nM in rat small airways. Indacaterol has the highest intrinsic efficacy of 53% in rat small airways and 73% in human small airways. Indacaterol (QAB149) (6.7 μg/kg) inhibits 5-HT-induced bronchoconstriction with a maximal effect of 85% in the conscious guinea pig. Indacaterol (QAB149) (12.5 μg/kg) dose-dependently inhibits methacholine-induced bronchoconstriction with a maximal effect of 85% in the anesthetized rhesus monkey.

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