In Vitro Pharmacological Characterization of Vilanterol, a Novel Long-Actingβ₂-Adrenoceptor Agonist with 24-Hour Duration of Action

Vilanterol trifenatate (vilanterol) is a novel, long-acting β(2)-adrenoceptor (β(2)-AR) agonist with 24 h activity. In this study, we describe the preclinical pharmacological profile of vilanterol using radioligand binding and cAMP studies in recombinant assays as well as human and guinea pig tissue systems to characterize β(2)-AR binding and functional properties. Vilanterol displayed a subnanomolar affinity for the β(2)-AR that was comparable...