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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
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Prostanoid receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Prostanoid Receptors [73]) are activated by the endogenous ligands prostaglandins PGD2, PGE1, PGE2 , PGF2α, PGH2, prostacyclin [PGI2] and thromboxane A2. Measurement of the potency of PGI2 and thromboxane A2 is hampered by their instability in physiological salt solution; they are often replaced by cicaprost and U46619, respectively, in receptor characterization studies.
DP1 receptor
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DP2 receptor
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EP1 receptor
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EP2 receptor
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EP3 receptor
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EP4 receptor
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FP receptor
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IP receptor
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TP receptor
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* Key recommended reading is highlighted with an asterisk
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Subcommittee members:
Xavier Norel (Chairperson)
Lucie Clapp
Akos Heinemann
Yukihiko Sugimoto, Ph.D.
Chengcan Yao |
Other contributors:
Richard M. Breyer
Robert A. Coleman
Mark Giembycz
Rebecca Hills
Robert L. Jones
Shuh Narumiya
Roy Pettipher
Mohib Uddin
David F. Woodward |
Database page citation (select format):
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2019) The Concise Guide to PHARMACOLOGY 2019/20: G protein-coupled receptors. Br J Pharmacol. 176 Issue S1: S21-S141.
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Whilst cicaprost is selective for IP receptors, it does exhibit moderate agonist potency at EP4 receptors [1]. Apart from IP receptors, iloprost also binds to EP1 receptors.
The EP1 agonist 17-phenyl-ω-trinor-PGE2 also shows agonist activity at EP3 and EP4 receptors [15,61]. Butaprost and SC46275 may require de-esterification within tissues to attain full agonist potency. There is evidence for subtypes of FP [30] and TP receptors [27,43]. mRNA for the EP3 receptor undergoes alternative splicing to produce variants which can interfere with signalling [42] or generate complex patterns of G-protein (Gi/o, Gq/11, Gs and G12,13) coupling (e.g. [26,41]). The number of EP3 receptor (protein) variants are variable depending on species, with five in human, three in rat and three in mouse. Putative receptor(s) for prostamide F (which as yet lack molecular correlates) and which preferentially recognize PGF2-1-ethanolamide and its analogues (e.g. Bimatoprost) have been identified, together with moderate-potency antagonists (e.g. AGN 211334) [72].
The free acid form of AL-12182, AL12180, used in in vitro studies, has a EC50 of 15nM which is the concentration of the compound giving half-maximal stimulation of inositol phosphate turnover in HEK-293 cells expressing the human FP receptor [48].
References given alongside the TP receptor agonists I-BOP [37] and STA2 [6] use human platelets as the source of TP receptors for competition radio-ligand binding assays to determine the indicated activity values.
Pharmacological evidence for a second IP receptor, denoted IP2, in the central nervous system [60,67] and in the BEAS-2B human airway epithelial cell line [71] is available. This receptor is selectively activated by 15R-17,18,19,20-tetranor-16-m-tolyl-isocarbacyclin (15R-TIC) and 15R-Deoxy 17,18,19,20-tetranor-16-m-tolyl-isocarbacyclin (15-deoxy-TIC). However, molecular biological evidence for an IP2 subtype is currently lacking.