Prostanoid receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Prostanoid Receptors [74]) are activated by the endogenous ligands prostaglandins PGD₂, PGE₁, PGE₂ , PGF_2α, PGH₂, prostacyclin [PGI₂] and thromboxane A₂. Differences and similarities between human and rodent prostanoid receptor orthologues, and their specific roles in pathophysiologic conditions are reviewed in [42]. 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.

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 [15,62]. 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 [27,44]. mRNA for the EP₃ receptor undergoes alternative splicing to produce variants which can interfere with signalling [43] or generate complex patterns of G-protein (G_i/o, G_q/11, G_s and G_12,13) 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) [73].

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 [49].

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 [61,68] and in the BEAS-2B human airway epithelial cell line [72] 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.

* Key recommended reading is highlighted with an asterisk

Gomez I, Foudi N, Longrois D, Norel X. (2013) The role of prostaglandin E2 in human vascular inflammation. Prostaglandins Leukot Essent Fatty Acids, 89 (2-3): 55-63. [PMID:23756023]

Jones RL, Giembycz MA, Woodward DF. (2009) Prostanoid receptor antagonists: development strategies and therapeutic applications. Br J Pharmacol, 158 (1): 104-45. [PMID:19624532]

Nakahata N. (2008) Thromboxane A2: physiology/pathophysiology, cellular signal transduction and pharmacology. Pharmacol Ther, 118 (1): 18-35. [PMID:18374420]

* Norel X, Sugimoto Y, Ozen G, Abdelazeem H, Amgoud Y, Bouhadoun A, Bassiouni W, Goepp M, Mani S, Manikpurage HD et al.. (2020) International Union of Basic and Clinical Pharmacology. CIX. Differences and Similarities between Human and Rodent Prostaglandin E₂ Receptors (EP1-4) and Prostacyclin Receptor (IP): Specific Roles in Pathophysiologic Conditions. Pharmacol Rev, 72 (4): 910-968. [PMID:32962984]

* Woodward DF, Jones RL, Narumiya S. (2011) International union of basic and clinical pharmacology. LXXXIII: classification of prostanoid receptors, updating 15 years of progress. Pharmacol Rev, 63 (3): 471-538. [PMID:21752876]

1. Abramovitz M, Adam M, Boie Y, Carrière M, Denis D, Godbout C, Lamontagne S, Rochette C, Sawyer N, Tremblay NM et al.. (2000) The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim Biophys Acta, 1483 (2): 285-93. [PMID:10634944]

2. Abramovitz M, Boie Y, Nguyen T, Rushmore TH, Bayne MA, Metters KM, Slipetz DM, Grygorczyk R. (1994) Cloning and expression of a cDNA for the human prostanoid FP receptor. J Biol Chem, 269 (4): 2632-6. [PMID:8300593]

3. af Forselles KJ, Root J, Clarke T, Davey D, Aughton K, Dack K, Pullen N. (2011) In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP₂ receptor antagonist. Br J Pharmacol, 164 (7): 1847-56. [PMID:21595651]

4. Amano H, Hayashi I, Endo H, Kitasato H, Yamashina S, Maruyama T, Kobayashi M, Satoh K, Narita M, Sugimoto Y et al.. (2003) Host prostaglandin E(2)-EP3 signaling regulates tumor-associated angiogenesis and tumor growth. J Exp Med, 197 (2): 221-32. [PMID:12538661]

5. An S, Yang J, Xia M, Goetzl EJ. (1993) Cloning and expression of the EP2 subtype of human receptors for prostaglandin E2. Biochem Biophys Res Commun, 197 (1): 263-70. [PMID:8250933]

6. Armstrong RA, Humphrey PP, Lumley P. (1993) Characteristics of the binding of [3H]-GR32191 to the thromboxane (TP-) receptor of human platelets. Br J Pharmacol, 110 (2): 539-47. [PMID:8242228]

7. Bastien L, Sawyer N, Grygorczyk R, Metters KM, Adam M. (1994) Cloning, functional expression, and characterization of the human prostaglandin E2 receptor EP2 subtype. J Biol Chem, 269 (16): 11873-7. [PMID:8163486]

8. Benyahia C, Boukais K, Gomez I, Silverstein A, Clapp L, Fabre A, Danel C, Leséche G, Longrois D, Norel X. (2013) A comparative study of PGI2 mimetics used clinically on the vasorelaxation of human pulmonary arteries and veins, role of the DP-receptor. Prostaglandins Other Lipid Mediat, 107: 48-55. [PMID:23850788]

9. Birrell MA, Maher SA, Buckley J, Dale N, Bonvini S, Raemdonck K, Pullen N, Giembycz MA, Belvisi MG. (2013) Selectivity profiling of the novel EP2 receptor antagonist, PF-04418948, in functional bioassay systems: atypical affinity at the guinea pig EP2 receptor. Br J Pharmacol, 168 (1): 129-38. [PMID:22747912]

10. Bley KR, Bhattacharya A, Daniels DV, Gever J, Jahangir A, O'Yang C, Smith S, Srinivasan D, Ford AP, Jett MF. (2006) RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists. Br J Pharmacol, 147 (3): 335-45. [PMID:16331286]

11. Boie Y, Rushmore TH, Darmon-Goodwin A, Grygorczyk R, Slipetz DM, Metters KM, Abramovitz M. (1994) Cloning and expression of a cDNA for the human prostanoid IP receptor. J Biol Chem, 269 (16): 12173-8. [PMID:7512962]

12. Boie Y, Sawyer N, Slipetz DM, Metters KM, Abramovitz M. (1995) Molecular cloning and characterization of the human prostanoid DP receptor. J Biol Chem, 270 (32): 18910-6. [PMID:7642548]

13. Cirillo R, Tos EG, Page P, Missotten M, Quattropani A, Scheer A, Schwarz MK, Chollet A. (2007) Arrest of preterm labor in rat and mouse by an oral and selective nonprostanoid antagonist of the prostaglandin F2alpha receptor (FP). Am J Obstet Gynecol, 197 (1): 54.e1-9. [PMID:17618756]

14. Davis TL, Sharif NA. (2000) Pharmacological characterization of [(3)H]-prostaglandin E(2) binding to the cloned human EP(4) prostanoid receptor. Br J Pharmacol, 130: 1919-1926. [PMID:10952683]

15. Foudi N, Kotelevets L, Gomez I, Louedec L, Longrois D, Chastre E, Norel X. (2011) Differential reactivity of human mammary artery and saphenous vein to prostaglandin E(2) : implication for cardiovascular grafts. Br J Pharmacol, 163 (4): 826-34. [PMID:21323896]

16. Foudi N, Kotelevets L, Louedec L, Leséche G, Henin D, Chastre E, Norel X. (2008) Vasorelaxation induced by prostaglandin E2 in human pulmonary vein: role of the EP4 receptor subtype. Br J Pharmacol, 154 (8): 1631-9. [PMID:18516068]

17. Ganesh T, Jiang J, Shashidharamurthy R, Dingledine R. (2013) Discovery and characterization of carbamothioylacrylamides as EP2 selective antagonists. ACS Med Chem Lett, 4 (7): 616-621. [PMID:23914286]

18. Giles H, Leff P, Bolofo ML, Kelly MG, Robertson AD. (1989) The classification of prostaglandin DP-receptors in platelets and vasculature using BW A868C, a novel, selective, and potent competitive antagonist. Br J Pharmacol, 96: 291-300. [PMID:2924081]

19. Grygorczyk R, Abramovitz M, Boie Y, Bastien L, Adam M. (1995) Detection of adenylate cyclase-coupled receptors in Xenopus oocytes by coexpression with cystic fibrosis transmembrane conductance regulator. Anal Biochem, 227: 27-31. [PMID:7545356]

20. Hata AN, Zent R, Breyer MD, Breyer RM. (2003) Expression and molecular pharmacology of the mouse CRTH2 receptor. J Pharmacol Exp Ther, 306 (2): 463-70. [PMID:12721327]

21. Hirata T, Narumiya S. (2011) Prostanoid receptors. Chem Rev, 111 (10): 6209-30. [PMID:21819041]

22. Honda A, Sugimoto Y, Namba T, Watabe A, Irie A, Negishi M, Narumiya S, Ichikawa A. (1993) Cloning and expression of a cDNA for mouse prostaglandin E receptor EP2 subtype. J Biol Chem, 268 (11): 7759-62. [PMID:8385118]

23. Jugus MJ, Jaworski JP, Patra PB, Jin J, Morrow DM, Laping NJ, Edwards RM, Thorneloe KS. (2009) Dual modulation of urinary bladder activity and urine flow by prostanoid EP3 receptors in the conscious rat. Br J Pharmacol, 158 (1): 372-81. [PMID:19486006]

24. Juteau H, Gareau Y, Labelle M, Sturino CF, Sawyer N, Tremblay N, Lamontagne S, Carrière MC, Denis D, Metters KM. (2001) Structure-activity relationship of cinnamic acylsulfonamide analogues on the human EP3 prostanoid receptor. Bioorg Med Chem, 9 (8): 1977-84. [PMID:11504634]

25. Kirihara T, Taniguchi T, Yamamura K, Iwamura R, Yoneda K, Odani-Kawabata N, Shimazaki A, Matsugi T, Shams N, Zhang JZ. (2018) Pharmacologic Characterization of Omidenepag Isopropyl, a Novel Selective EP2 Receptor Agonist, as an Ocular Hypotensive Agent. Invest Ophthalmol Vis Sci, 59 (1): 145-153. [PMID:29332128]

26. Kotani M, Tanaka I, Ogawa Y, Usui T, Mori K, Ichikawa A, Narumiya S, Yoshimi T, Nakao K. (1995) Molecular cloning and expression of multiple isoforms of human prostaglandin E receptor EP3 subtype generated by alternative messenger RNA splicing: multiple second messenger systems and tissue-specific distributions. Mol Pharmacol, 48 (5): 869-79. [PMID:7476918]

27. Krauss AH, Woodward DF, Gibson LL, Protzman CE, Williams LS, Burk RM, Gac TS, Roof MB, Abbas F, Marshall K et al.. (1996) Evidence for human thromboxane receptor heterogeneity using a novel series of 9,11-cyclic carbonate derivatives of prostaglandin F2 alpha. Br J Pharmacol, 117 (6): 1171-80. [PMID:8882612]

28. Kuwano K, Hashino A, Asaki T, Hamamoto T, Yamada T, Okubo K, Kuwabara K. (2007) 2-[4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy]-N-(methylsulfonyl)acetamide (NS-304), an orally available and long-acting prostacyclin receptor agonist prodrug. J Pharmacol Exp Ther, 322 (3): 1181-8. [PMID:17545310]

29. Leduc M, Breton B, Galés C, Le Gouill C, Bouvier M, Chemtob S, Heveker N. (2009) Functional selectivity of natural and synthetic prostaglandin EP4 receptor ligands. J Pharmacol Exp Ther, 331 (1): 297-307. [PMID:19584306]

30. Liljebris C, Selén G, Resul B, Stjernschantz J, Hacksell U. (1995) Derivatives of 17-phenyl-18,19,20-trinorprostaglandin F2 alpha isopropyl ester: potential antiglaucoma agents. J Med Chem, 38 (2): 289-304. [PMID:7830272]

31. Longrois D, Gomez I, Foudi N, Topal G, Dhaouadi M, Kotelevets L, Chastre E, Norel X. (2012) Prostaglandin E₂ induced contraction of human intercostal arteries is mediated by the EP₃ receptor. Eur J Pharmacol, 681 (1-3): 55-9. [PMID:22342278]

32. Luker T, Bonnert R, Brough S, Cook AR, Dickinson MR, Dougall I, Logan C, Mohammed RT, Paine S, Sanganee HJ et al.. (2011) Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981. Bioorg Med Chem Lett, 21 (21): 6288-92. [PMID:21944852]

33. Lumley P, White BP, Humphrey PP. (1989) GR32191, a highly potent and specific thromboxane A2 receptor blocking drug on platelets and vascular and airways smooth muscle in vitro. Br J Pharmacol, 97 (3): 783-94. [PMID:2527074]

34. Machwate M, Harada S, Leu CT, Seedor G, Labelle M, Gallant M, Hutchins S, Lachance N, Sawyer N, Slipetz D et al.. (2001) Prostaglandin receptor EP(4) mediates the bone anabolic effects of PGE(2). Mol Pharmacol, 60 (1): 36-41. [PMID:11408598]

35. Maruyama T, Asada M, Shiraishi T, Ishida A, Egashira H, Yoshida H, Maruyama T, Ohuchida S, Nakai H, Kondo K et al.. (2001) Design and synthesis of a highly selective EP4-receptor agonist. Part 1: 3,7-dithiaPG derivatives with high selectivity. Bioorg Med Chem Lett, 11 (15): 2029-31. [PMID:11454473]

36. Mathiesen JM, Christopoulos A, Ulven T, Royer JF, Campillo M, Heinemann A, Pardo L, Kostenis E. (2006) On the mechanism of interaction of potent surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2. Mol Pharmacol, 69 (4): 1441-53. [PMID:16418339]

37. Mayeux PR, Morinelli TA, Williams TC, Hazard ES, Mais DE, Oatis JE, Baron DA, Halushka PV. (1991) Differential effect of pH on thromboxane A2/prostaglandin H2 receptor agonist and antagonist binding in human platelets. J Biol Chem, 266 (21): 13752-8. [PMID:1830308]

38. Monneret G, Cossette C, Gravel S, Rokach J, Powell WS. (2003) 15R-methyl-prostaglandin D2 is a potent and selective CRTH2/DP2 receptor agonist in human eosinophils. J Pharmacol Exp Ther, 304 (1): 349-55. [PMID:12490611]

39. Morinelli TA, Oatis JE, Okwu AK, Mais DE, Mayeux PR, Masuda A, Knapp DR, Halushka PV. (1989) Characterization of an 125I-labeled thromboxane A2/prostaglandin H2 receptor agonist. J Pharmacol Exp Ther, 251: 557-562. [PMID:2530338]

40. Naka M, Mais DE, Morinelli TA, Hamanaka N, Oatis Jr JE, Halushka PV. (1992) 7-[(1R,2S,3S,5R)-6,6-dimethyl-3-(4- iodobenzenesulfonylamino)bicyclo[3.1.1]hept-2-yl]-5(Z)-heptenoic acid: a novel high-affinity radiolabeled antagonist for platelet thromboxane A2/prostaglandin H2 receptors. J Pharmacol Exp Ther, 262 (2): 632-7. [PMID:1386885]

41. Negishi M, Irie A, Sugimoto Y, Namba T, Ichikawa A. (1995) Selective coupling of prostaglandin E receptor EP3D to Gi and Gs through interaction of alpha-carboxylic acid of agonist and arginine residue of seventh transmembrane domain. J Biol Chem, 270 (27): 16122-7. [PMID:7608175]

42. Norel X, Sugimoto Y, Ozen G, Abdelazeem H, Amgoud Y, Bouhadoun A, Bassiouni W, Goepp M, Mani S, Manikpurage HD et al.. (2020) International Union of Basic and Clinical Pharmacology. CIX. Differences and Similarities between Human and Rodent Prostaglandin E₂ Receptors (EP1-4) and Prostacyclin Receptor (IP): Specific Roles in Pathophysiologic Conditions. Pharmacol Rev, 72 (4): 910-968. [PMID:32962984]

43. Okuda-Ashitaka E, Sakamoto K, Ezashi T, Miwa K, Ito S, Hayaishi O. (1996) Suppression of prostaglandin E receptor signaling by the variant form of EP1 subtype. J Biol Chem, 271 (49): 31255-61. [PMID:8940129]

44. Raychowdhury MK, Yukawa M, Collins LJ, McGrail SH, Kent KC, Ware JA. (1994) Alternative splicing produces a divergent cytoplasmic tail in the human endothelial thromboxane A2 receptor. J Biol Chem, 269 (30): 19256-61. [PMID:8034687]

45. Royer JF, Schratl P, Lorenz S, Kostenis E, Ulven T, Schuligoi R, Peskar BA, Heinemann A. (2007) A novel antagonist of CRTH2 blocks eosinophil release from bone marrow, chemotaxis and respiratory burst. Allergy, 62 (12): 1401-9. [PMID:17714552]

46. Sando T, Usui T, Tanaka I, Mori K, Sasaki Y, Fukuda Y, Namba T, Sugimoto Y, Ichikawa A, Narumiya S et al.. (1994) Molecular cloning and expression of rat prostaglandin E receptor EP2 subtype. Biochem Biophys Res Commun, 200 (3): 1329-33. [PMID:8185583]

47. Sawyer N, Cauchon E, Chateauneuf A, Cruz RP, Nicholson DW, Metters KM, O'Neill GP, Gervais FG. (2002) Molecular pharmacology of the human prostaglandin D2 receptor, CRTH2. Br J Pharmacol, 137 (8): 1163-72. [PMID:12466225]

48. Sharif NA, Davis TL. (2002) Cloned human EP1 prostanoid receptor pharmacology characterized using radioligand binding techniques. J Pharm Pharmacol, 54 (4): 539-47. [PMID:11999132]

49. Sharif NA, McLaughlin MA, Kelly CR, Xu S, Crider JY, Williams GW, Parker JL. (2006) Preclinical pharmacology of AL-12182, a new ocular hypotensive 11-oxa prostaglandin analog. J Ocul Pharmacol Ther, 22 (5): 291-309. [PMID:17076623]

50. Shichijo M, Sugimoto H, Nagao K, Inbe H, Encinas JA, Takeshita K, Bacon KB, Gantner F. (2003) Chemoattractant receptor-homologous molecule expressed on Th2 cells activation in vivo increases blood leukocyte counts and its blockade abrogates 13,14-dihydro-15-keto-prostaglandin D2-induced eosinophilia in rats. J Pharmacol Exp Ther, 307 (2): 518-25. [PMID:12975488]

51. Siegl AM, Smith JB, Silver MJ, Nicolaou KC, Ahern D. (1979) Selective binding site for [3H]prostacyclin on platelets. J Clin Invest, 63 (2): 215-20. [PMID:372237]

52. Stillman BA, Breyer MD, Breyer RM. (1999) Importance of the extracellular domain for prostaglandin EP(2) receptor function. Mol Pharmacol, 56 (3): 545-51. [PMID:10462542]

53. Stitham J, Arehart E, Gleim SR, Li N, Douville K, Hwa J. (2007) New insights into human prostacyclin receptor structure and function through natural and synthetic mutations of transmembrane charged residues. Br J Pharmacol, 152 (4): 513-22. [PMID:17704830]

54. Sturino CF, O'Neill G, Lachance N, Boyd M, Berthelette C, Labelle M, Li L, Roy B, Scheigetz J, Tsou N et al.. (2007) Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524). J Med Chem, 50 (4): 794-806. [PMID:17300164]

55. Sugimoto H, Shichijo M, Okano M, Bacon KB. (2005) CRTH2-specific binding characteristics of [3H]ramatroban and its effects on PGD2-, 15-deoxy-Delta12, 14-PGJ2- and indomethacin-induced agonist responses. Eur J Pharmacol, 524 (1-3): 30-7. [PMID:16256979]

56. Suzawa T, Miyaura C, Inada M, Maruyama T, Sugimoto Y, Ushikubi F, Ichikawa A, Narumiya S, Suda T. (2000) The role of prostaglandin E receptor subtypes (EP1, EP2, EP3, and EP4) in bone resorption: an analysis using specific agonists for the respective EPs. Endocrinology, 141 (4): 1554-9. [PMID:10746663]

57. Swayne GT, Maguire J, Dolan J, Raval P, Dane G, Greener M, Owen DA. (1988) Evidence for homogeneity of thromboxane A2 receptor using structurally different antagonists. Eur J Pharmacol, 152 (3): 311-9. [PMID:2975605]

58. Syed NI, Jones RL. (2015) Assessing the agonist profiles of the prostacyclin analogues treprostinil and naxaprostene, particularly their DP₁ activity. Prostaglandins Leukot Essent Fatty Acids, 95: 19-29. [PMID:25542069]

59. Sykes D, Bradley M, Riddy D, Willard L, Powell-Herlaar E, Sandham D, Watson S, Bauer C, Dubois G, Charlton S. (2014) QAW039, a slowly dissociating CRTh2 antagonist with potential for improved clinical efficacy. Eur Respir J, 44 (Supl 58): 4074.

60. Sykes DA, Bradley ME, Riddy DM, Willard E, Reilly J, Miah A, Bauer C, Watson SJ, Sandham DA, Dubois G et al.. (2016) Fevipiprant (QAW039), a Slowly Dissociating CRTh2 Antagonist with the Potential for Improved Clinical Efficacy. Mol Pharmacol, 89 (5): 593-605. [PMID:26916831]

61. Takechi H, Matsumura K, Watanabe Y, Kato K, Noyori R, Suzuki M, Watanabe Y. (1996) A novel subtype of the prostacyclin receptor expressed in the central nervous system. J Biol Chem, 271 (10): 5901-6. [PMID:8621463]

62. Theiler A, Konya V, Pasterk L, Maric J, Bärnthaler T, Lanz I, Platzer W, Schuligoi R, Heinemann A. (2016) The EP1/EP3 receptor agonist 17-pt-PGE₂ acts as an EP4 receptor agonist on endothelial barrier function and in a model of LPS-induced pulmonary inflammation. Vascul Pharmacol, 87: 180-189. [PMID:27664754]

63. Theis JG, Dellweg H, Perzborn E, Gross R. (1992) Binding characteristics of the new thromboxane A2/prostaglandin H2 receptor antagonist [3H]BAY U 3405 to washed human platelets and platelet membranes. Biochem Pharmacol, 44 (3): 495-503. [PMID:1387312]

64. Torisu K, Kobayashi K, Iwahashi M, Nakai Y, Onoda T, Nagase T, Sugimoto I, Okada Y, Matsumoto R, Nanbu F et al.. (2004) Discovery of a new class of potent, selective, and orally active prostaglandin D2 receptor antagonists. Bioorg Med Chem, 12 (20): 5361-78. [PMID:15388164]

65. Torres D, Paget C, Fontaine J, Mallevaey T, Matsuoka T, Maruyama T, Narumiya S, Capron M, Gosset P, Faveeuw C et al.. (2008) Prostaglandin D2 inhibits the production of IFN-gamma by invariant NK T cells: consequences in the control of B16 melanoma. J Immunol, 180 (2): 783-92. [PMID:18178816]

66. Ulven T, Kostenis E. (2005) Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem, 48 (4): 897-900. [PMID:15715457]

67. Watanabe K, Kawamori T, Nakatsugi S, Ohta T, Ohuchida S, Yamamoto H, Maruyama T, Kondo K, Ushikubi F, Narumiya S et al.. (1999) Role of the prostaglandin E receptor subtype EP1 in colon carcinogenesis. Cancer Res, 59 (20): 5093-6. [PMID:10537280]

68. Watanabe Y, Matsumura K, Takechi H, Kato K, Morii H, Björkman M, Långström B, Noyori R, Suzuki M, Watanabe Y. (1999) A novel subtype of prostacyclin receptor in the central nervous system. J Neurochem, 72 (6): 2583-92. [PMID:10349870]

69. Whittle BJ, Silverstein AM, Mottola DM, Clapp LH. (2012) Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonist. Biochem Pharmacol, 84 (1): 68-75. [PMID:22480736]

70. Wilson RJ, Giblin GM, Roomans S, Rhodes SA, Cartwright KA, Shield VJ, Brown J, Wise A, Chowdhury J, Pritchard S et al.. (2006) GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): a novel, potent and selective prostanoid EP4 receptor antagonist. Br J Pharmacol, 148 (3): 326-39. [PMID:16604093]

71. Wilson RJ, Giles H. (2005) Piglet saphenous vein contains multiple relaxatory prostanoid receptors: evidence for EP4, EP2, DP and IP receptor subtypes. Br J Pharmacol, 144 (3): 405-15. [PMID:15655509]

72. Wilson SM, Sheddan NA, Newton R, Giembycz MA. (2011) Evidence for a second receptor for prostacyclin on human airway epithelial cells that mediates inhibition of CXCL9 and CXCL10 release. Mol Pharmacol, 79 (3): 586-95. [PMID:21173040]

73. Woodward DF, Carling RW, Cornell CL, Fliri HG, Martos JL, Pettit SN, Liang Y, Wang JW. (2008) The pharmacology and therapeutic relevance of endocannabinoid derived cyclo-oxygenase (COX)-2 products. Pharmacol Ther, 120 (1): 71-80. [PMID:18700152]

74. Woodward DF, Jones RL, Narumiya S. (2011) International union of basic and clinical pharmacology. LXXXIII: classification of prostanoid receptors, updating 15 years of progress. Pharmacol Rev, 63 (3): 471-538. [PMID:21752876]

75. Wright DH, Metters KM, Abramovitz M, Ford-Hutchinson AW. (1998) Characterization of the recombinant human prostanoid DP receptor and identification of L-644,698, a novel selective DP agonist. Br J Pharmacol, 123 (7): 1317-24. [PMID:9579725]

76. Wright DH, Nantel F, Metters KM, Ford-Hutchinson AW. (1999) A novel biological role for prostaglandin D2 is suggested by distribution studies of the rat DP prostanoid receptor. Eur J Pharmacol, 377 (1): 101-15. [PMID:10448933]

77. Yamane S, Karakawa T, Nakayama S, Nagai K, Moriyuki K, Neki S, Suto F, Kambe T, Hirota Y, Kawabata K. (2015) IOP-Lowering Effect of ONO-9054, A Novel Dual Agonist of Prostanoid EP3 and FP Receptors, in Monkeys. Invest Ophthalmol Vis Sci, 56 (4): 2547-52. [PMID:25788650]

78. Young RN, Billot X, Han Y, Slipetz DA, Chauret N, Belley M, Metters K, Mathieu MC, Greig GM, Denis D, Girard M. (2004) Discovery and Synthesis of a Potent, Selective and Orally Bioavailable EP4 Receptor Agonist. Heterocycles, 64 (1): 437-446.

Subcommittee members: Xavier Norel (Chairperson) INSERM U1148 Laboratory for Vascular Translational Science (LVTS) Bichat-Claude Bernard Hospital 46, rue Henri Huchard 75877 Paris Cedex 18 France Lucie Clapp Professor of Vascular Physiology Institute of Cardiovascular Science Floor 3, Rayne Building University College London 5 University Street London, WC1E 6JF Akos Heinemann Otto Loewi Research Center (for Vascular Biology, Immunology and Inflammation) Division of Pharmacology Lehrstuhlinhaber/Lehrstuhlinhaberin Universitätsplatz 4 8010 Graz Yukihiko Sugimoto, Ph.D. Department of Pharmaceutical Biochemistry Graduate School of Pharmaceutical Sciences Kumamoto University 5-1, Oe-Honmachi, Chuo-ku Kumamoto 862-0973 JAPAN Chengcan Yao Edinburgh Medical School: Clinical Sciences Centre for Inflammation Research University of Edinburgh, UK

Other contributors: Richard M. Breyer Department of Medicine Vanderbilt University School of Medicine Nashville TN USA Robert A. Coleman Pharmagene Laboratories 2A Orchard Road Royston SG8 5HD UK Mark Giembycz Snyder Institute for Chronic Diseases Health Research Innovation Centre 4AA08 3280 Hospital Drive NW Calgary, T2N 4N1 AB Canada Rebecca Hills (Past curator) Robert L. Jones Strathclyde Institude of Pharmacy and Biomedical Sciences University of Strathclyde The John Arbuthnott Building 27 Taylor Street Glasgow G4 0NR UK Shuh Narumiya Department of Pharmacology Kyoto University Faculty of Medicine Yoshida Sakyo-ku Kyoto 606 Japan Roy Pettipher Atopix Therapeutics Ltd The Innovation Centre 99 Park Drive Milton Park Abingdon UK Mohib Uddin AstraZeneca R&D BioPharmaceuticals Gothenburg, SE-431 83 Sweden David F. Woodward Biological Sciences Allergan PO Box 19534 2525 Dupont Drive Irvine CA 92713-9534 USA