Role of A_2B adenosine receptor signaling in adenosine-dependent pulmonary inflammation and injury
J. Clin. Invest. Chun-Xiao Sun, et al. 116:2173 doi:10.1172/JCI27303 [Go to this article.]

Figure 1
Pharmacological characterization of CVT-6883 as an A_2B AR antagonist. (A) Structure of CVT-6883. (B) Competition of CVT-6883 for specific radioligand binding to membranes prepared from CHO cells overexpressing the A₁AR or A₃AR or from HEK cells over-expressing the A_2AAR or A_2BAR. Increasing concentrations of CVT-6883 were used to displace the specific binding of selective receptor radioligands: ³H-CPX (A₁AR antagonist; 0.45 nM), ³H-ZM241385 (A_2AAR antagonist; 1.6 nM), ³H-ZM241385 (A_2BAR antagonist; 9.3 nM), or ³H-MRE3008F20 (A₃AR antagonist; 0.63 nM). Data are presented as mean ± SEM percent specific binding of control from 6 determinations. (C) Concentration response curves of NECA-induced increases in cAMP in the absence or presence of increasing concentrations of CVT-6883. Mouse NIH/3T3 cells were treated with NECA (1 nM to 100 μM) in the absence or presence of increasing concentrations of CVT-6883, and cAMP accumulation was measured. Data are mean ± SEM from 3 experiments performed in duplicate. Inset is the Schild plot. DR – 1, concentration ratio minus 1.