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

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3607-10. doi: 10.1016/j.bmcl.2004.03.084.

Abstract

MRE 2029-F20 [N-benzo[1,3]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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetamides / chemical synthesis*
  • Acetamides / pharmacology
  • Adenosine A2 Receptor Antagonists*
  • Allyl Compounds / chemistry
  • Animals
  • Benzoquinones / chemistry
  • Binding, Competitive
  • CHO Cells
  • Cricetinae
  • Humans
  • Purines / chemical synthesis*
  • Purines / chemistry
  • Purines / pharmacology
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / chemistry
  • Pyrazoles / pharmacology
  • Radioligand Assay
  • Receptor, Adenosine A2B / metabolism
  • Tritium / chemistry
  • Xanthine / chemistry

Substances

  • Acetamides
  • Adenosine A2 Receptor Antagonists
  • Allyl Compounds
  • Benzoquinones
  • N-benzo(1,3)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
  • Purines
  • Pyrazoles
  • Receptor, Adenosine A2B
  • Tritium
  • Xanthine