Synthesis and use of FSCPX, an irreversible adenosine A1 antagonist, as a 'receptor knock-down' tool

Bioorg Med Chem Lett. 2001 Mar 26;11(6):815-8. doi: 10.1016/s0960-894x(01)00069-5.

Abstract

A new preparative synthetic route for the irreversible adenosine A1 antagonist 8-cyclopentyl-3-N-[3-((3-(4-fluorosulphonyl)benzoyl)-oxy)-propyl]-1-N-propyl-xanthine (FSCPX, 1) is described. The availability of ample amounts of the irreversible antagonist FSCPX allowed us to use FSCPX as a research tool for adenosine A1 receptors in in vivo experiments. After verification of the irreversible antagonistic function of FSCPX in in vitro experiments, FSCPX was used successfully as a 'receptor knock-down' tool in in vivo experiments on conscious rats.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding Sites
  • Cyclic AMP / metabolism
  • Heart Rate / drug effects
  • In Vitro Techniques
  • Purinergic P1 Receptor Antagonists*
  • Rats
  • Xanthines / chemical synthesis*
  • Xanthines / chemistry
  • Xanthines / pharmacology

Substances

  • Purinergic P1 Receptor Antagonists
  • Xanthines
  • 8-cyclopentyl-3-(3-((4-(fluorosulfonyl)benzoyl)oxy)propyl)-1-propylxanthine
  • Cyclic AMP