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

Autor: van Muijlwijk-Koezen JE; Leiden/Amsterdam Center for Drug Research, Department of Pharmacochemistry, Vrije Universiteit, Amsterdam, The Netherlands. muylwyk@chem.vu.nl, Timmerman H, van der Sluis RP, van de Stolpe AC, Menge WM, Beukers MW, van der Graaf PH, de Groote M, IJzerman AP
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2001 Mar 26; Vol. 11 (6), pp. 815-8.
DOI: 10.1016/s0960-894x(01)00069-5
Abstrakt: 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.
Databáze: MEDLINE