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. Author manuscript; available in PMC: 2013 Jun 1.

Published in final edited form as: Biochem Pharmacol. 2012 Mar 1;83(11):1552–1561. doi: 10.1016/j.bcp.2012.02.019

A) Test of known AR ligands (MRS1220, Cl-IB-MECA, NECA and DPCPX). Competitive binding assay was performed using CHO cells expressing the hA₃AR incubated with 5 nM MRS5449 and increasing concentrations of the adenosine receptor ligands for 90 min at 37 °C. The K_i values are (nM): 3.46 ± 0.8; 27.7 ± 6.3; 149 ± 13 and 1320 ± 60; respectively. Results are expressed as mean ± S.E. (n=3). B) Detailed displacement curve of Cl-IB-MECA using MRS5449 as a tracer. Competitive binding assay was performed using CHO cells expressing hA₃AR incubated with 5 nM MRS5449 and increasing concentrations of the Cl-IB-MECA for 90 min at 37 °C. The displacement curve can be best fitted in a two-site model. Results are expressed as mean ± S.E. (n=2).

A) Test of known AR ligands (MRS1220, Cl-IB-MECA, NECA and DPCPX). Competitive binding assay was performed using CHO cells expressing the hA₃AR incubated with 5 nM MRS5449 and increasing concentrations of the adenosine receptor ligands for 90 min at 37 °C. The K_i values are (nM): 3.46 ± 0.8; 27.7 ± 6.3; 149 ± 13 and 1320 ± 60; respectively. Results are expressed as mean ± S.E. (n=3). B) Detailed displacement curve of Cl-IB-MECA using MRS5449 as a tracer. Competitive binding assay was performed using CHO cells expressing hA₃AR incubated with 5 nM MRS5449 and increasing concentrations of the Cl-IB-MECA for 90 min at 37 °C. The displacement curve can be best fitted in a two-site model. Results are expressed as mean ± S.E. (n=2).