Description
AH 6809 is an EP and DP receptor antagonist with nearly equal affinity for the cloned human EP
1, EP
2, EP
3-
III, and DP
1 receptors. AH 6809 blocks the PGE
2-
induced accumulation of cAMP in COS cells transfected with the human EP
2 receptor. It also blocks the accumulation of Ca
2+ in
Xenopus oocytes expressing the human EP
1 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 EP
2 receptor, but also acts as a weak ligand at the murine EP
1 and DP
1 receptors. In whole human platelets, AH 6809 is an effective antagonist of the antiaggregatory actions of PGD
2, but not PGI
2, with an EC
50 of about 5 x 10
−5 M.
