产品描述:
Indacaterol is a long-acting and selective β2-adrenergic receptor (β2-AR) agonist (EC50 = 8.71 nM for increasing intracellular cAMP levels in vitro).{32131} It is selective for β2-ARs over β1- and β3-ARs (Kis = 43.6, 616.6, and 3,311.3 nM, respectively). Indacaterol inhibits bronchoconstriction induced by serotonin (5-HT; Item No. 14332) in conscious guinea pigs with a maximal effect of 85% when administered intratracheally at a dose of 6.7 µg/kg. It also inhibits bronchoconstriction induced by methacholine (Item No. 23092) in rhesus monkeys with a maximal effect of 75% when administered via nebulization at a dose of 12.5 mg/kg. Formulations containing indacaterol have been used alone, and in combination with glycopyrrolate, in the treatment of chronic obstructive pulmonary disease.