Skip to main content
. Author manuscript; available in PMC: 2014 Jan 1.
Published in final edited form as: Bioorg Med Chem Lett. 2012 Nov 5;23(1):26–36. doi: 10.1016/j.bmcl.2012.10.112

Figure 3.

Figure 3

Screening of AR ligands using fluorescent techniques.
  1. Fluorescence binding assay using the Alexa Fluor 488-tagged A2AAR antagonist MRS5346 52 (20 nM) as a tracer, HEK-A2AAR membranes and FP (60 min incubation at 30 °C).
  2. FMC binding assay using potent and selective fluorescent A3AR antagonist MRS5449 (5 nM) on intact CHO-A3AR cells (90 min incubation at 37 °C). Reproduced from Kozma et al. with permission.6 Antagonists showed similar binding affinity as determined in radioligand binding assay using cell membranes. However, agonists show altered affinity toward A3ARs on intact cells, which may be due to multiple agonist binding sites of the receptor.