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

Bioorg Med Chem Lett. 2000 Feb 7;10(3):209-11. doi: 10.1016/s0960-894x(99)00674-5.

Abstract

The synthesis and the preliminary biological evaluation of the first high affinity radioligand antagonist for the human A3 adenosine receptor, named [3H]-MRE 3008-F20 are reported. [3H]-MRE 3008-20 bound human A3 receptors expressed in CHO cells with K(D) and Bmax value of 0.82 +/- 0.08 nM and 297 +/- 28 fmol/mg of protein, respectively. [3H]-MRE 3008-F20 represents a useful tool for a further characterization of A3 adenosine receptor subtype.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CHO Cells
  • Cricetinae
  • Humans
  • Phenylurea Compounds / chemical synthesis*
  • Phenylurea Compounds / metabolism
  • Phenylurea Compounds / pharmacology*
  • Purinergic P1 Receptor Antagonists*
  • Radioligand Assay
  • Receptor, Adenosine A3
  • Receptors, Purinergic P1 / metabolism
  • Recombinant Proteins / antagonists & inhibitors
  • Recombinant Proteins / metabolism
  • Triazoles / chemical synthesis*
  • Triazoles / metabolism
  • Triazoles / pharmacology*
  • Tritium

Substances

  • MRE 3008-F20
  • Phenylurea Compounds
  • Purinergic P1 Receptor Antagonists
  • Receptor, Adenosine A3
  • Receptors, Purinergic P1
  • Recombinant Proteins
  • Triazoles
  • Tritium