Prostanoid receptors are activated by the endogenous ligands prostaglandin (PG) D2, PGE2, PGF2α, PGH2, prostacyclin (PGI2) and thromboxane A2. Cyclooxygenase (COX) converts arachidonic acid to PGH2, from which the other prostaglandins are synthesized.
Prostanoid Receptor Agonists |
|
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Cat. No. | Product Name / Activity |
4180 | Beraprost sodium |
Potent prostacyclin IP receptor agonist | |
4027 | 16,16-Dimethyl Prostaglandin E2 |
Synthetic prostaglandin E2 (Cat. No. 2296) derivative; regulates HSC development | |
2989 | Epoprostenol |
Endogenous IP receptor agonist | |
2297 | Misoprostol |
Cytoprotective PGE1 analog | |
2296 | Prostaglandin E2 |
Promotes HSCs expansion; increases HSCs engraftment; also endogenous prostaglandin | |
4214 | Prostaglandin F2α |
Naturally-occurring prostanoid; potent vasoconstrictor | |
3351 | Selexipag |
Selective prostacyclin IP1 receptor agonist | |
3049 | Sulprostone |
EP3 and EP1 receptor agonist | |
4069 | TCS 2510 |
Selective EP4 agonist | |
5349 | Treprostinil |
Potent prostacyclin (PGI2) analog | |
1932 | U 46619 |
Potent, stable thromboxane A2 (TP) receptor agonist | |
Prostanoid Receptor Antagonists |
|
Cat. No. | Product Name / Activity |
0671 | AH 6809 |
EP1 and EP2 receptor antagonist | |
5701 | AMG 853 |
Potent dual CRTH2 and prostaglandin D2 (PGD2) receptor antagonist | |
2732 | BAY-u 3405 |
Dual TP/DP2 (CRTH2) receptor antagonist | |
5327 | BGC 20-1531 hydrochloride |
High affinity and selective EP4 antagonist | |
6240 | DG 041 |
Potent and selective EP3 antagonist; antiplatelet and antithrombotic | |
4668 | GW 627368 |
Selective EP4 receptor competitive antagonist | |
2514 | L-161,982 |
Selective EP4 receptor antagonist | |
3342 | L-798,106 |
Potent and highly selective EP3 antagonist | |
7343 | Laropiprant New |
Potent and selective prostaglandin D2 receptor antagonist | |
5406 | ONO 8130 |
EP1 receptor antagonist | |
3565 | ONO AE3 208 |
High affinity and selective EP4 antagonist | |
4818 | PF 04418948 |
Potent and selective EP2 receptor antagonist | |
4268 | Ro 1138452 hydrochloride |
Selective prostacyclin IP receptor antagonist | |
5568 | S 18886 |
Potent thromboxane A2 (TP) antagonist | |
1206 | SC 19220 |
Selective EP1 receptor antagonist | |
3758 | SC 51089 |
Selective EP1 receptor antagonist | |
2791 | SC 51322 |
Potent EP1 receptor antagonist | |
5052 | TG 4-155 |
High affinity and selective EP2 receptor antagonist | |
Other |
|
Cat. No. | Product Name / Activity |
1620 | Alprostadil |
Prostaglandin. Vasodilator and antiplatelet agent in vivo |
Prostanoid receptors are activated by the endogenous ligands prostaglandin (PG) D2, PGE2, PGF2α, PGH2, prostacyclin (PGI2) and thromboxane A2. Cyclooxygenase (COX) converts arachidonic acid to PGH2, from which the other prostaglandins are synthesized. Prostanoid receptors are a family of nine G-protein-coupled receptors that have distinct tissue distributions and actions.
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Gene | Species | Gene Symbol | Gene Accession No. | Protein Accession No. |
---|---|---|---|---|
EP1 | Human | PTGER1 | NM_000955 | P34995 |
Mouse | Ptger1 | NM_013641 | P35375 | |
Rat | Ptger1 | NM_013100 | P70597 | |
EP2 | Human | PTGER2 | NM_000956 | P43116 |
Mouse | Pyry2 | NM_008964 | Q62053 | |
Rat | Ptger2 | NM_031088 | Q62928 | |
EP3 | Human | PTGER3 | NM_000957 | P43115 |
Mouse | Ptger3 | NM_011196 | P30557 | |
Rat | Ptger3 | NM_012704 | P34980 | |
EP4 | Human | PTGER4 | NM_000958 | P35408 |
Mouse | Ptger4 | NM_008965 | P32240 | |
Rat | Ptger4 | NM_032076 | P43114 | |
TP | Human | TBXA2R | NM_201636 | P21731 |
Mouse | Tbxa2r | NM_009325 | P30987 | |
Rat | Tbxa2r | NM_017054 | P34978 | |
FP | Human | PTGFR | NM_000959 | P43088 |
Mouse | Ptgfr | NM_008966 | P43117 | |
Rat | Ptgfr | NM_013115 | P43118 | |
IP | Human | PTGIR | NM_000960 | P43119 |
Mouse | Ptgir | NM_008967 | P43252 | |
Rat | Ptgir | NM_001077644 | P43253 | |
DP | Human | PTGDR | NM_000953 | Q13258 |
Mouse | Ptgdr | NM_008962 | P70263 | |
Rat | Ptgdr | NM_022241 | O35932 |
Receptor Subtype | EP1 | EP2 | EP3 | EP4 |
---|---|---|---|---|
Transduction Mechanism | Gq → ↑ PI hydrolysis/Ca2+ | Gs → ↑ cAMP | Various (splice variants), mainly ↓ cAMP | Gs → ↑ cAMP |
Agonist Potencies | PGE2 > PGF2, PGI2 > PGD2, TXA2 | PGE2 > PGF2, PGI2 > PGD2, TXA2 | PGE2 > PGF2, PGI2 > PGD2, TXA2 | PGE2 > PGF2, PGI2 > PGD2, TXA2 |
Receptor Distribution | Kidney, lung (mouse) | Lung, placenta (human), uterus, lung, ileum, liver, thymus, spleen (mouse) | Kidney, uterus, stomach, brain, thymus, lung, spleen (mouse), kidney, pancreas, uterus, heart, liver, testis, ovary (human) | Ileum, thymus, spleen, lung, heart, stomach, uterus (mouse) |
Tissue Functions | GI contraction, tracheal contraction (guinea-pig), gastric fundus contraction | Bronchodilatation (guinea-pig, cat), myometrial inhibition (human,baboon), vasodepression (cat, guinea-pig) | Inhibition of gastric acid secretion (human, dog, rat), myometrial stimulation (human, cat,rat, hamster) | Vasodilatation (dog), bronchodilatation (rat) |
Receptor Subtype | DP | FP | IP | TP |
---|---|---|---|---|
Transduction Mechanism | Gs → ↑ cAMP | Gq → ↑ PI hydrolysis/Ca2+ |
Gs → ↑ cAMP ↑ PI hydrolysis/Ca2+ |
Gq → ↑ PI hydrolysis/Ca2+ |
Agonist Potencies | PGD2 >> PGE2 > PGF2 > PGI2, TXA2 | PGF2 > PGD2 > PGE2 > PGI2, TXA2 | PGI2 >> PGD2 ,PGE2, PGF2 > TXA2 | TXA2 = PGH2 >> PGD2, PGE2, PGF2, PGI2 |
Receptor Distribution | Ileum, lung, stomach, uterus (mouse) | Corpus luteum, kidney, lung, heart, stomach (mouse), overy, small intestine, prostate, spleen, testis (human) | Aorta, lung, heart, kidney (human), thymus, spleen (mouse), NTS, dorsal horn (rat) | Thymus, spleen, lung, kidney, heart, uterus (mouse) |
Tissue Functions | Inhibition of platelet aggregation | Luteolysis | Vasodepression, inhibition of platelet aggregation | Vaso- and bronchoconstriction, platelet aggregation, myometrial stimulation |
IUPHAR Compendium of receptor characterization and classification. (2000) 2nd Edition. IUPHAR Media. Breyer et al (2001) Prostanoid receptors: subtypes and signaling. Ann.Rev.Pharmacol.Toxicol. 41 661.