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 (Kis = 43.6, 616.6, and 3,311.3 nM, respectively). Indacaterol inhibits bronchoconstriction induced by serotonin 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).