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

J E van Muijlwijk-Koezen; H Timmerman; R P van der Sluis; A C van de Stolpe; W M Menge; M W Beukers; P H van der Graaf; M de Groote; A P IJzerman

doi:10.1016/s0960-894x(01)00069-5

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.

Authors

J E van Muijlwijk-Koezen¹, H Timmerman, R P van der Sluis, A C van de Stolpe, W M Menge, M W Beukers, P H van der Graaf, M de Groote, A P IJzerman

Affiliation

¹ Leiden/Amsterdam Center for Drug Research, Department of Pharmacochemistry, Vrije Universiteit, Amsterdam, The Netherlands. [email protected]

PMID: 11277527
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