[1044516-17-7]    

Synonyms : (R)-5-(2-((6-(2,2-difluoro-2-phenylethoxy)hexyl)amino)-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one heminaphthalene-1,5-disulfonate

Applications : Abediterol is a novel potent, long-acting inhaled β(2)-adrenoceptor agonist in development for the treatment of asthma and chronic obstructive pulmonary disease. Abediterol shows subnanomolar affinity for the human β(2)-adrenoceptor and a functional selectivity over β(1)-adrenoceptors higher than that of formoterol and indacaterol in both a cellular model with overexpressed human receptors and isolated guinea pig tissue. Abediterol is a full agonist at the human β(2)-adrenoceptor (E(max) = 91 ± 5% of the maximal effect of isoprenaline). The potency and onset of action that abediterol shows in isolated human bronchi (EC(50) = 1.9 ± 0.4 nM; t½ onset = 7-10 min) is not significantly different from that of formoterol, but its duration of action (t½ ∼ 690 min) is similar to that of indacaterol.

References : Aparici M. et al.: Eur. J Pharmacol., 770, 61-9, 2016; Montuschi P. et al.: J. Med Chem., 58(10), 4131-64, 2015; Singh D. et al.: BMC Pulm Med., 14, 176, 2014; Beier J. et al.: Respir Med., 108(10), 1424-9, 2014; Timmer W. et al.: J. Clin Pharmacol., 54(12), 1347-53, 2014; Fuso L. et al.: Curr Med Chem., ;20(12), 1477-95, 2013; Cazzola M. et al.: Am J Respir Crit Care Med., 187(7):690-6, 2013; Aparici M. et al.: J. Pharmacol Exp Ther., 342(2), 497-509, 2012.

Storage : Keep container tightly closed under nitrogen or argon and refrigerate for long-term shelf life.

Caution : In case of contact with skin or eyes, rinse immediately with plenty of water and seek medical advice. Wear suitable protective clothing and gloves.