Characterization of a prostanoid EP3-receptor in guinea-pig aorta: partial agonist action of the non-prostanoid ONO-AP-324
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Abstract1 Contraction of guinea-pig isolated aorta induced by the prostaglandin E analogue sulprostone (1-400 nM) has a lower maximum response (40%) than that of phenylephrine or U-46619 (TP-receptor agonist). A prostanoid EP3-receptor subtype is involved based on agonist potency ranking: equi-effective molar ratios (EMR) are sulprostone (EC(50)similar to 23 nM) 1.0, SC-46275 0.11, misoprostol 2.2, gemeprost 3.3, PGE(2) 5.4, 17-phenyl PGE(2) 6.0, GR-63799 8.9. GR-63799, which contains a bulky ester group, is relatively more potent on neuronal EP3 preparations than on the aorta.
All Author(s) ListJones RL, Qian YM, Chan KM, Yim APC
Journal nameBritish Journal of Pharmacology
Volume Number125
Issue Number6
Pages1288 - 1296
LanguagesEnglish-United Kingdom
Keywordsarterial smooth muscle; G(i)-coupled second messenger systems; L-type Ca2+-channel blockers; non-prostanoid EP3 agonists; non-prostanoid prostacyclin mimetics; prostaglandin E-2; prostanoid EP3-receptors; sulprostone
Web of Science Subject CategoriesPharmacology & Pharmacy; PHARMACOLOGY & PHARMACY

Last updated on 2020-06-06 at 00:17