Synthetic procedure for the preparation of novel potent and selective A3 adenosine receptor radioligands

Nucleosides Nucleotides Nucleic Acids. 2001 Apr-Jul;20(4-7):775-9. doi: 10.1081/NCN-100002428.

Abstract

2-Phenylethynyladenosine and its N6-methyl derivative were synthesized and evaluated in binding assays at human adenosine receptors stably transfected on CHO cells. Results showed that the N6-methyl-2-phenylethynyladenosine is endowed with very high affinity and selectivity at A3 receptor subtype. Hence, an alternative procedure for the synthesis of tritiated N6-methyl-2-phenylethynyladenosine was set up to introduce tritiated methylamine in the final step.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine / analogs & derivatives*
  • Adenosine / chemistry*
  • Adenosine / metabolism
  • Animals
  • CHO Cells
  • Cricetinae
  • Humans
  • Isotope Labeling / methods
  • Ligands
  • Receptor, Adenosine A3
  • Receptors, Purinergic P1 / metabolism*
  • Substrate Specificity
  • Tritium

Substances

  • Ligands
  • N6-methyl-2-phenylethynyladenosine
  • Receptor, Adenosine A3
  • Receptors, Purinergic P1
  • Tritium
  • Adenosine