Indacaterol-d
3 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 β
2-adrenergic receptor (β
2-AR) agonist (EC
50 = 8.71 nM for increasing intracellular cAMP levels
in vitro).
1 It is selective for β
2-ARs over β
1- and β
3-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.
