TABLE 2

Biochemical characteristics, endogenous ligands, signaling pathways, and representative agonists and antagonists of prostanoid receptors

Data from Jones et al., 1995; Tsuboi et al., 2002; Nagata and Hirai, 2003; Hata and Breyer, 2004; Norel, 2007; Jones et al., 2009.

PRMMEndogenous LigandsG-ProteinSecond MessengerAgonistsAntagonists
DP140.012 (M)
40.276 (H)		PGD2 PGJ2GsMainly ↑ cAMP Other: ↑ Ca2+BW245CaAH6809 BWA868Ca,b,c MK-0524 (laropiprant)a,b ONO-AE3-237a
DP2 (CRTH2)43 (H)PGD2
15-Deoxy-PGJ2		Gi
Gq?		Mainly ↓ cAMP
    Other: ↑Ca2+, PLC, PI3K, MAPK		13,14-Dihydro-15-keto-PGD2a 15-(R)-methyl-PGD2aBAY-u3405 (ramatroban)
    TM-30642a,b
    TM-30089a,b
EP142.966 (M)
41.858 (H)		PGE2
8-iso-PGE2		Gq?↑ Ca2+Iloprost,b ONO-DI-004a 17-Phenyl-PGE2b SulprostonebAH6809
    ONO-8713a,b
    SC51322b
EP240.478 (M)
39.38 (H)		PGE2GsMainly ↑ cAMP
    Other: EGFR transactivation, GSK-3/β-catenin		AH13205
    Butaprosta
    16,16-Dimethyl-PGE2b
    ONO-AE1-259,a PGE1b		AH6809
EP340.077 (M)
40.5–43.315 (H)		PGE2
8-iso-PGE2		Gi
Gq
Gs		Mainly ↓ cAMP
    Other: ↑ IP3/ DAG, cAMP		11-Deoxy-PGE1b
    GR-63799Xa,b
    Iloprost, M&B-28767b
    ONO-AE248,a PGE1b
    SC-46275a
    Sulprostoneb		DG041b
    L826266
    ONO-AE3-240b
EP456.157 (M)
53.115 (H)		PGE2GsMainly ↑ cAMP
    Other: PI3K, ERK1/2, GSK-3/β-catenin		11-Deoxy-PGE1b
    L-902688
    Misoprostol
    ONO-AE-329a,b		AH23848
    EP4Aa
    L161982b
    ONO-AE3-227b
FP40.077 (M)PGF2α
PGD2
PGE2		GqMainly ↑ IP3/DAG
    Other: ERK, EGFR trans-activation, β-catenin		Cloprostenol
    Fluprostenola,b
    Latanoprosta
    17-Phenyl-PGE2		AS604872
IP44.722 (M)
40.06 (H)		PGI2
PGE2		Gs
Gq
Gi		Mainly ↑ cAMP, Rac/PAK1, ↓ Rho-A
    Other: ↑ IP3/DAG, ↓ cAMP
    ↓Akt-1, ↓↑MAPK		Beraprostb
    Carbacyclin
    Cicaprostb
    Iloprostb
    Isocarbacyclinb
    PGE1		RO1138452a,b
    RO3244794a,b
TP37.114 (M)
37.429 (H)		TXA2
PGH2
8-iso-PGF2α		Gq
G12/13
Gi
Gs		Mainly ↑ IP3/DAG, ↑ Rho-A
    Other: ↓ cAMP
    ↑ cAMP
    ↑ MAPK		GR-32191 (vapiprost)b
    I-BOPb
    STA2a,b
    U-46619a		AH23848b
    BAYu3405 (ramatroban)b
    GR32191 (vapiprost)b

  • AH13205, trans-2-(4-(1-hydroxyhexyl)phenyl)-5-oxocyclopentaneheptanoic acid; AH23848, (4Z)-7-[(rel-1S,2S,5R)-5-((1,1′-biphenyl-4-yl)methoxy)-2-(4-morpholinyl)-3-oxocyclopentyl]-4-heptenoic acid; AH23848, 7-(5-(((1,1-biphenyl)-4-yl)methoxy)-2-(4-morpholinyl)-3-oxocyclopentyl)-4-heptanoic acid; AS604872, (2S)-3-((1,1′-biphenyl)-4-ylsulfonyl)-N-((R)-phenyl(2-pyridinyl)methyl)-1,3-thiazolidine-2-carboxamide; BW245C, 3-((2-cyclohexyl-2-hydroxyethylidene) amino)-2,5-dioxo-4-imidazolidineheptanoic acid; BWA868C, 3-((2-cyclohexyl-2-hydroxyethyl)amino)-2,5-dioxo-1-(phenylmethyl)-4-imidazolidineheptanoic acid; DG041, 2,3-dichlorothiophene-5-sulfonic acid, 3-[1-(2,4-dichlorobenzyl)-5-fluoro-3-methyl-1H-indol-7-yl]acryloylamide; GR-63799X, (4-benzamidophenyl)-(Z)-7-[(1R,2R,3R)-3-hydroxy-2-[(2R)-2-hydroxy-3-phenoxypropoxy]-5-oxocyclopentyl]hept-5-enoate; GSK-3, glycogen synthase kinase-3; (H), human; I-BOP, [1S-[1α,2α(Z),3β(1E,3S*),4α]]-7-[3-[3-hydroxy-4-(4-iodophenoxy)-1-butenyl]-7-oxabi-cyclo[2.2.1]hept-2-yl]5-heptenoic acid; IP3, inositol trisphosphate; L161982, N-{[4′-({3-butyl-5-oxo-1-[2-(trifluoromethyl)phenyl]-1,5-dihydro-4H-1,2,4-triazol-4-yl}methyl)biphenyl-2-yl] sulfonyl}-3-methylthiophene-2-carboxamide; L826266, [(2E)-N-[(5-bromo-2-methoxyphenyl)-sulfonyl]-3-[5-chloro-2-(2-naphthylmethyl)phenyl]acrylamide; L-902688, 5R-[(1E)-4,4-difluoro-3R-hydroxy-4-phenylbut-1-en-1-yl]-1-[6-(1H-tertrazol-5-yl)hexyl]pyrrolidin-2-one; (M), mouse; M&B-28767, 7-[(1R,2R)-2-[(E,3R)-3-hydroxy-4-(phenoxy)but-1-enyl]-5-oxocyclopentyl]heptanoic acid; MM, molecular mass of cloned receptor; ONO-8713, (E)-3-[4-[[2-(furan-2-ylsulfonyl-(2-methylpropyl)amino)-5-(trifluoromethyl)phenoxy]methyl]phenyl]prop-2-enoic acid; ONO-AE1-259, 9-deoxy-9-chloro-15-deoxy-16-hydroxy-17,17-trimethylene-19,20-didehydroprostaglandin E2; ONO-AE-248, 16S-9-deoxy-9β-chloro-15-deoxy-16-hydroxy-17,17-trimethylene-19, 20-didehydro-prostaglandin F2; ONO-AE3-227, Hata and Breyer (2004); ONO-AE3-237, Jones et al. (2009); ONO-AE3-240, 2-[2-{[4-methyl-2-(1-naphthyl)pentanoyl]amino}-4-(1H-pyrazol-1-ylmethyl)benzyl]benzoic acid; ONO-AE-329, 2-[3-[(1R,2S,3R)-3-hydroxy-2-[(E,3S)-3-hydroxy-5-[2-(methoxymethyl)phenyl]pent-1-enyl]-5-oxocyclopentyl]sulfanylpropylsulfanyl]acetic acid; ONO-DI-004, 17S-2,5-ethano-6-oxo-17,20-dimethyl prostaglandin E1; PI3K, phosphatidylinositol 3-kinase; SC-46275, methyl 7-(2β-(6-(1-cyclo-pentyl-yl)-4R-hydroxy-4-methyl-1E,5E-hexadienyl)-3α-hydroxy-5-oxo-1R,1α-cyclopentyl)-4Z-heptenoate; SC51322, 8-chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 2-[3-2-(furanylmethyl)thio]-1-oxopropyl]hydrazide; STA2, 9,11-epithio-11,12-methanothromboxane A2; TM-30089, (+)-3-[[(4-fluorophenyl)sulfonyl]methylamino]-1,2,3,4-tetrahydro-9H-carbazole-9-acetic acid; TM-30642, Jones et al. (2009).

  • ↵a High receptor selectivity.

  • ↵b High affinity (agonist binding Ki ≤ 25 in mouse tissue or pA2 ≥ 8 in different species).

  • ↵c Partial agonist activity.