EP Receptor Selective Ligands

structures of some compounds that are active at EP2 receptors are shown in Fig. 6.6. Several compounds have been described that seem to be specific EP2 receptor agonists. The first compound identified, but later found to possess some EP3 receptor activity as well, was the PGE, analog, AY23626 (228). Misoprostol and 19(R)-OH PGE, (229) are also EP2 receptor agonists, but the former is more potent at EP3 receptors (222) and the latter at EP, receptors (116). Despite a lack of absolute selectivity, both these agents have been useful tools in preparations lacking EP3 receptors. More specific for the EP, receptor are AH13205 (230) and butaprost (TR4979) (231). Butap-rost, although not possessing great potency, is highly selective for the EP2 receptor subtype

Table 6.5 Potencies of Some EP, Receptor Agonists and Antagonists


Equieffective Concentration Relative to PGE, (=1.0)


17-phenyl-trinor PGE,



I Antagonists




4-6 la pA2

228 60,116


226,228 226,228 63

"Partial agonist. 6pKi value.

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