CVT-6883 is an adenosine A2B receptor antagonist (Ki = 22 nM).1 It is selective for adenosine A2B over adenosine A1, A2A, and A3 receptors (Kis = 1,940, 3,280, and 1,070 nM, respectively), as well as a panel of 84 receptors, ion channels, transporters, and enzymes at 10 ?M. CVT-6883 (6 mg/kg) decreases allergen challenge-induced bronchoalveolar lavage fluid (BALF) eosinophil and lymphocyte infiltration and airway reactivity in a mouse model of allergic asthma.2 It also decreases fibrosis in the non-infarct zone, improves ejection fractions, and reduces ventricular tachycardia in a rat model of myocardial infarction.3
1.Elzein, E., Kalla, R.V., Li, X., et al.Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseasesJ. Med. Chem.51(7)2267-2278(2008) 2.Mustafa, S.J., Nadeem, A., Fan, M., et al.Effect of a specific and selective A2B adenosine receptor antagonist on adenosine agonist AMP and allergen-induced airway responsiveness and cellular influx in a mouse model of asthmaJ. Pharmacol. Exp. Ther.320(3)1246-1251(2007) 3.Zhang, H., Zhong, H., Everett, T.H., 4th, et al.Blockade of A2B adenosine receptor reduces left ventricular dysfunction and ventricular arrhythmias 1 week after myocardial infarction in the rat modelHeart Rhythm11(1)101-109(2014)