Premium
In vitro characterization of prostanoid EP‐receptors in the non‐pregnant human myometrium
Author(s) -
Senior J.,
Marshall K.,
Sangha R.,
Baxter G.S.,
Clayton J.K.
Publication year - 1991
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1991.tb12244.x
Subject(s) - agonist , myometrium , prostanoid , prostaglandin e2 receptor , receptor , endocrinology , medicine , chemistry , partial agonist , receptor antagonist , prostaglandin , pharmacology , biology , antagonist , uterus
1 Prostaglandin receptors of the PGE type have been characterized in the non‐pregnant human myometrium in vitro according to the scheme of Coleman et al . (1984) by use of the agonists PGE 2 , sulprostone, rioprostil, AY23626, butaprost, misoprostol, 16,16‐dimethylprostaglandin E 2 , enprostil and iloprost, and, the antagonist AH6809. 2 All prostanoids tested were active in non‐pregnant human myometrium either as stimulators and/or inhibitors of spontaneous activity or both. Biphasic responses to PGE 2 indicate that at least two receptor types of the EP‐receptor exist, one mediating relaxation and the other mediating contraction. 3 Further evidence for the EP‐receptor mediating excitation and relaxation was provided by the action of the EP 2 ‐/EP 3 ‐receptor selective prostanoids rioprostil, AY23626 and misoprostol, and the EP 1 ‐/EP 2 ‐receptor selective agonist 16,16‐dimethylprostaglandin E 2 . 4 Butaprost, an EP 2 ‐receptor selective agonist, produced potent inhibition of spontaneous activity in the tissue which was generally longer‐lasting than that evoked by the natural prostanoid PGE 2 . 5 The EP 1 ‐/EP 3 ‐receptor selective agonist sulprostone and the EP 3 ‐receptor agonist enprostil produced potent contractile responses supporting the presence of contractile EP 3 ‐receptors in the non‐pregnant human myometrium in vitro . 6 The EP 1 ‐/IP‐receptor selective agonist, iloprost, produced mixed responses in non‐pregnant human myometrium. The contractile response was inhibited by the EP 1 ‐receptor antagonist AH6809. However, responses to the EP 1 ‐/EP 3 ‐receptor selective agonist sulprostone were unaffected by AH6809 which may indicate that only a small population of EP 1 ‐receptors is present. 7 Therefore it would seem that a heterogeneous population of EP‐receptors is present in the non‐pregnant human myometrium.