3H]-MRE 2029-F20, a selective antagonist radioligand for the human A2B adenosine receptors

MRE 2029-F20 N-benzo1,3]dioxol-5-yl-2-5-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-1-methyl-1H-pyrazol-3-yloxy]-acetamide] is a selective antagonist ligand of A2B adenosine receptors. For use as a radioligand, 1,3-diallyl-xanthine, the precursor of 3H]-MRE 2029-F20, was synthesized, and tritiated on the allyl groups. 3H]-MRE 2029-F20 bound to human A2B receptors expressed in CHO cells showed a KD value of 1.65+/-0.10 nM and Bmax value of 36+/-4 fmol/mg protein. 3H]-MRE2029-F20 represents a useful tool for the pharmacological characterization of human A2B adenosine receptor subtype.