Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20:: the first high affinity radioligand antagonist for the human A3 adenosine receptors

The synthesis and the preliminary biological evaluation of the first high affinity radioligand antagonist for the human A(3) adenosine receptor, named [H-3]-MRE 3008-F20 are reported. [H-3]-MRE 3008-20 bound human A(3) receptors expressed in CHO cells with K-D and B-max value of 0.82 +/- 0.08 nM and 297 +/- 28 fmol/mg of protein, respectively. [H-3]-MRE 3008-F20 represents a useful tool for a further characterization of A(3) adenosine receptor subtype. (C) 2000 Elsevier Science Ltd. All rights reserved.