6-ISOPROPOXY-9-XANTHONE-2-CARBOXYLIC ACID

Description

AH 6809 is an EP and DP receptor antagonist with nearly equal affinity for the cloned human EP₁, EP₂, EP₃-III, and DP₁ receptors. AH 6809 blocks the PGE₂-induced accumulation of cAMP in COS cells transfected with the human EP₂ receptor. It also blocks the accumulation of Ca²⁺ in Xenopus oocytes expressing the human EP₁ receptor. In the human and guinea pig, the activity profile of AH 6809 is similar to that of SC-19220, but it is somewhat more potent. In the mouse, AH 6809 has the highest affinity for the EP₂ receptor, but also acts as a weak ligand at the murine EP₁ and DP₁ receptors. In whole human platelets, AH 6809 is an effective antagonist of the antiaggregatory actions of PGD₂, but not PGI₂, with an EC₅₀ of about 5 x 10⁻⁵ M.

Uses

AH-6809 is a prostaglandin E2 receptor antagonist.

Definition

ChEBI: 9-oxo-6-propan-2-yloxy-2-xanthenecarboxylic acid is a member of xanthones.

Biological Activity

Antagonist at prostaglandin EP 1 (pA 2 = 6.8 ) and EP 2 (K i = 350 nM) receptors. Also weakly inhibits DP receptors (pA 2 = 4.45).

storage

Store at RT

References

1) Coleman in Prostaglandins and Related Substances: A Practical Approach; ILR Press, Oxford and Washington D.C. 1987, pg 267