Abstract
Rank order of agonist potency for activation of adenylate cyclase by the naturally occurring prostanoids PGE 2, PGF 2α, PGD 2, the stable PGI 2 analogue iloprost, and the TXA 2 mimetic U 46619, provides evidence for the existence of a distinct PGE-receptor on guinea-pig duodenal enterocytes. This PGE-receptor is likely to be of the EP 2-subtype since the specific EP 2-agonist 11-deoxy-PGE 1 stimulated adenylate cyclase activity with a 20-fold higher potency than the EP 1-agonist 17-phenyltrinor-PGE 2 and the EP 3-agonists MB 28767 and GR 63799. In addition, sulprostone (acting on both EP 1- and EP 3-receptors) was ineffective. Since the specific EP 1-antagonist SC 19220 did not inhibit PGE 2-stimulated adenylate cyclase activity, the involvement of EP 1-receptors could be further excluded. The synthetic prostaglandin E-analogues misoprostol and nocloprost stimulated adenylate cyclase almost identically, though they were about 10-fold less potent than the natural PGE 2.
Published Version
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