Vilanterol-d4 is intended for use as an internal standard for the quantification of vilanterol by GC- or LC-MS. Vilanterol is an ultra-long acting β2-adrenoceptor agonist (ultra-LABA) that has 1,000-fold selectivity for β2-over other β-receptors (EC50s = 398, 0.39, and 794 nM for β1, β2, and β3, respectively).1,2 In addition to its potency and selectivity, vilanterol is characterized by rapid onset of activity and prolonged duration of action.1,3
1.Cazzola, M., Calzetta, L., and Matera, M.G.β2-adrenoceptor agonists: Current and future directionBr. J. Pharmacol.163(1)4-17(2011) 2.Mach, R.H., Nader, M.A., Ehrenkaufer, R.L., et al.Comparison of two fluorine-18 labeled benzamide derivatives that bind reversibly to dopamine D2 receptors: In vitro binding studies and positron emission tomographySynapse24(4)322-333(1996) 3.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 approachJ. Med. Chem.53(11)4522-4530(2010)