2021249-10-3

Vilanterol-d₄ is intended for use as an internal standard for the quantification of vilanterol by GC- or LC-MS. Vilanterol is a long-acting agonist of the β₂-adrenergic receptor (β₂-AR).¹ It selectively induces cAMP accumulation in CHO cells expressing the β₂-AR over the β₁- and β₃-ARs (EC₅₀ = 0.4, 398, and 794 nM for the human receptors, respectively). Vilanterol inhibits contractions induced by electrical stimulation in isolated superfused guinea pig trachea strips. It inhibits bronchospasms induced by histamine in guinea pigs when administered via nebulization (EC₅₀ = 30 μM). Formulations containing vilanterol, in combination with fluticasone, have been used in the treatment of chronic obstructive pulmonary disease (COPD) and asthma.

1. Procopiou, P.A., Barrett, V.J., Bevan, N.J., et al. Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: An antedrug approach J. Med. Chem. 53(11),4522-4530(2010).