6-isopropoxy-9-oxoxanthene-2-carboxylic acid (AH 6809), a human EP2 receptor antagonist

David F. Woodward; David J. Pepperl; Thomas H. Burkey; John W. Regan

doi:10.1016/0006-2952(95)02035-7

6-isopropoxy-9-oxoxanthene-2-carboxylic acid (AH 6809), a human EP₂ receptor antagonist

David F. Woodward, David J. Pepperl, Thomas H. Burkey, John W. Regan

Research output: Contribution to journal › Article › peer-review

101 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	1731-1733
Number of pages	3
Journal	Biochemical Pharmacology
Volume	50
Issue number	10
DOIs	https://doi.org/10.1016/0006-2952(95)02035-7
State	Published - Nov 9 1995

Keywords

AH 6809
G-protein coupled receptor
adenylyl cyclase
cAMP
prostaglandins

ASJC Scopus subject areas

Biochemistry
Pharmacology

Access to Document

10.1016/0006-2952(95)02035-7

Cite this

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title = "6-isopropoxy-9-oxoxanthene-2-carboxylic acid (AH 6809), a human EP2 receptor antagonist",

abstract = "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.",

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T1 - 6-isopropoxy-9-oxoxanthene-2-carboxylic acid (AH 6809), a human EP2 receptor antagonist

AU - Woodward, David F.

AU - Pepperl, David J.

AU - Burkey, Thomas H.

AU - Regan, John W.

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AB - 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.

KW - AH 6809

KW - G-protein coupled receptor

KW - adenylyl cyclase

KW - cAMP

KW - prostaglandins

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