2699828-16-3

Indacaterol-d₃ is intended for use as an internal standard for the quantification of indacaterol by GC- or LC-MS. Indacaterol is a long-acting and selective β₂-adrenergic receptor (β₂-AR) agonist (EC₅₀ = 8.71 nM for increasing intracellular cAMP levels in vitro).¹ It is selective for β₂-ARs over β₁- and β₃-ARs (K_is = 43.6, 616.6, and 3,311.3 nM, respectively). Indacaterol inhibits bronchoconstriction induced by serotonin (5-HT; ) 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 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.

1. Battram, C., Charlton, S.J., Cuenoud, B., et al. In vitro and in vivo pharmacological characterization of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one (indacaterol), a novel inhaled β₂ adrenoceptor agonist with a 24-h duration of action J. Pharmacol. Exp. Ther. 317(2),762-770(2006).