3H]-MRE 2029-F20, a selective antagonist radioligand for the human A 2B adenosine receptors

Abstract

MRE 2029-F20 [N-benzo[1,3]dioxol-5-yl-2-[5-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1 H-purin-8-yl)-1-methyl-1 H-pyrazol-3-yloxy]-acetamide] is a selective antagonist ligand of A 2B 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 A 2B receptors expressed in CHO cells showed a K D value of 1.65 ± 0.10 nM and B max value of 36 ± 4 fmol/mg protein. [ 3H]-MRE2029-F20 represents a useful tool for the pharmacological characterization of human A 2B adenosine receptor subtype.