Background:

Vilanterol trifenatate is a novel and selective agonist of β2-AR with a PEC50 value of 10.37±0.05 [1].

Vilanterol trifenatate is a novel long-acting β2-AR agonist (LABA) with 24h activity in development for inhaled once daily treatment. In the radioligand binding studies, Vilanterol trifenatate has shown the binding affinity in the one-affinity site model with pKD values of 9.44±0.07 and 10.82±0.12 in the presence Gpp(NH)p and absence Gpp(NH)p, respectively. In dissociation studies, Vilanterol trifenatate has been reported to bind from the β2-AR with a dissociation t1/2 value of 3.5 min in the presence of Gpp(NH)p. Vilanterol trifenatate has been found to have a good selectivity for β2-AR over the other β-AR receptor subtypes(β1and β3) with pEC50 values of 10.37±0.05, 6.98±0.03 and 7.36±0.03, respectively. Vilanterol trifenatate has exhibited at least 1000-fold selectivity over both β1-and β3-AR subtypes [1].

参考文献:
[1] Slack RJ1, Barrett VJ, Morrison VS, Sturton RG, Emmons AJ, Ford AJ, Knowles RG.In vitro pharmacological characterization of vilanterol, a novel long-acting β2-adrenoceptor agonist with 24-hour duration of action.J Pharmacol Exp Ther. 2013 Jan; 344(1):218-30.