1. Synthesis and use of FSCPX, an irreversible adenosine A1 antagonist, as a 'receptor knock-down' tool.
- Author
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van Muijlwijk-Koezen JE, Timmerman H, van der Sluis RP, van de Stolpe AC, Menge WM, Beukers MW, van der Graaf PH, de Groote M, and IJzerman AP
- Subjects
- Animals, Binding Sites, Cyclic AMP metabolism, Heart Rate drug effects, In Vitro Techniques, Rats, Xanthines chemistry, Xanthines pharmacology, Purinergic P1 Receptor Antagonists, Xanthines chemical synthesis
- 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.
- Published
- 2001
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