6-Isopropoxy-9-oxoxanthene-2-carboxylic acid (AH 6809), a human EP2 receptor antagonist.
On studying the interaction of various ligands with the pharmacologically defined, recombinant human EP2 receptor (Regan et al., Mol Pharmacol 46: 213-220, 1994), we discovered that the putative EP1 receptor antagonist 6-isopropoxy-9-oxoxanthene-2-carboxylic acid (AH 6809) also has affinity for the human EP2 receptor. Moreover, AH 6809 behaved as an EP2 receptor antagonist and inhibited prostaglandin E2 (PGE2)-stimulated increases in cyclic AMP. These findings have significant implications for studies that employ AH 6809 to determine the pharmacological basis of PGE2-induced responses in human cells and tissues.
Woodward
D F
DF
Department of Biosciences (RD-2C), Allergan Inc., Irvine, CA 92713, USA.
Pepperl
D J
DJ
Burkey
T H
TH
Regan
J W
JW
D000818:Animals; D001667:Binding, Competitive; D002478:Cells, Cultured; D000242:Cyclic AMP / Q000096:biosynthesis; D015232:Dinoprostone / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D011448:Prostaglandin Antagonists / Q000494:pharmacology* / Q000633:toxicity; D018078:Receptors, Prostaglandin E / Q000037:antagonists & inhibitors* / Q000378:metabolism; D014316:Tritium; D014966:Xanthenes / Q000378:metabolism / Q000494:pharmacology*; D044004:Xanthones
D011448:Prostaglandin Antagonists; D018078:Receptors, Prostaglandin E; D014966:Xanthenes; D044004:Xanthones; D014316:Tritium; C053876:6-isopropoxy-9-oxoxanthene-2-carboxylic acid; D000242:Cyclic AMP; D015232:Dinoprostone