Indacaterol-d₃

Indacaterol-d₃ is intended for use as an internal standard for the quantification of indacaterol (Item No. 20070) 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; 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.

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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).