Vilanterol displayed a subnanomolar affinity for the β(2)-AR that was comparable with that of salmeterol but higher than olodaterol, formoterol, and indacaterol. In cAMP functional activity studies, vilanterol demonstrated similar selectivity as salmeterol for β(2)- over β(1)-AR and β(3)-AR, but a significantly improved selectivity profile than formoterol and indacaterol. Vilanterol also showed a level of intrinsic efficacy that was comparable to indacaterol but significantly greater than that of salmeterol. In cellular cAMP production and tissue-based studies measuring persistence and reassertion, vilanterol had a persistence of action comparable with indacaterol and longer than formoterol. In addition, vilanterol demonstrated reassertion activity in both cell and tissue systems that was comparable with salmeterol and indacaterol but longer than formoterol.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
In vitro pharmacological characterization of vilanterol, a novel long-acting β2-adrenoceptor agonist with 24-hour duration of action.
Slack RJ, et al. J Pharmacol Exp Ther. 2013 Jan;344(1):218-30. PMID: 23131596.
The efficacy and safety of the novel long-acting β2 agonist vilanterol in patients with COPD: a randomized placebo-controlled trial.
Hanania NA, et al. Chest. 2012 Jul;142(1):119-27. PMID: 22241764.
|Related Adrenergic Receptor Products|
Norepinephrine is generally considered to be a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
Vibegron is a potent and selective beta 3 adrenergic receptor agonist.
L-755,507 is a very potent and selective β 3 partial agonist.
5-Iodotubercidin is a potent adenosine kinase inhibitor with IC50 of 26 nM. It inhibits nucleoside transporter, CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC.
Xylometazoline is an α-adrenoceptor agonist commonly used as nasal decongestant, exhibits highest potency at α2B-adrenoceptor subtype with EC50 of 99 μM.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.