Bioorganic & Medicinal Chemistry Letters 2001-03-26

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

Index: Bioorg. Med. Chem. Lett. 11 , 815, (2001)

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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.