Synthesis and use of FSCPX, an irreversible adenosine A1 antagonist, as a 'receptor knock-down' tool.
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.
van Muijlwijk-Koezen
J E
JE
Leiden/Amsterdam Center for Drug Research, Department of Pharmacochemistry, Vrije Universiteit, Amsterdam, The Netherlands. muylwyk@chem.vu.nl
Timmerman
H
H
van der Sluis
R P
RP
van de Stolpe
A C
AC
Menge
W M
WM
Beukers
M W
MW
van der Graaf
P H
PH
de Groote
M
M
IJzerman
A P
AP
D000818:Animals; D001665:Binding Sites; D000242:Cyclic AMP / Q000378:metabolism; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D058915:Purinergic P1 Receptor Antagonists; D051381:Rats; D014970:Xanthines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D058915:Purinergic P1 Receptor Antagonists; D014970:Xanthines; C100640:8-cyclopentyl-3-(3-((4-(fluorosulfonyl)benzoyl)oxy)propyl)-1-propylxanthine; D000242:Cyclic AMP