Top ▲

DP1 receptor

Click here for help

Target id: 338

Nomenclature: DP1 receptor

Family: Prostanoid receptors

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 359 14q22.1 PTGDR prostaglandin D2 receptor 5
Mouse 7 357 14 22.59 cM Ptgdr prostaglandin D receptor 16,19
Rat 7 357 15p14 Ptgdr prostaglandin D2 receptor 60
Previous and Unofficial Names Click here for help
DP1 | prostanoid DP receptor-like | PTGDR1 | prostaglandin D2 receptor (DP)
Database Links Click here for help
Specialist databases
GPCRdb pd2r_human (Hs), pd2r_mouse (Mm), pd2r_rat (Rn)
Other databases
Alphafold
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
PGD2
PGE1
PGE2
PGF
PGI2
PGJ2
Comments: PGD2 is the principal endogenous agonist
Potency order of endogenous ligands
PGD2 > PGE1 >> PGE2 > PGF > PGI2, thromboxane A2

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]PGD2 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Full agonist 7.9 – 9.5 pKd 57,59
pKd 7.9 – 9.5 (Kd 1.3x10-8 – 3x10-10 M) [57,59]
[3H]PGE2 Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure ? Agonist 7.5 – 7.9 pKd
pKd 7.5 – 7.9 (Kd 3.4x10-8 – 1.3x10-8 M)
Δ12-PGJ2 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.0 pKd 59
pKd 7.0 [59]
ZK110841 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.5 pKi 59
pKi 9.5 [59]
L-644,698 Small molecule or natural product Hs Full agonist 9.0 – 9.3 pKi 59-60
pKi 9.0 – 9.3 [59-60]
PGJ2 Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 9.0 pKi 59
pKi 9.0 [59]
BW 245C Small molecule or natural product Hs Full agonist 8.4 – 9.4 pKi 5,59-60
pKi 8.4 – 9.4 [5,59-60]
PGD2 Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 7.8 – 9.2 pKi 5,57,59-60
pKi 7.8 – 9.2 [5,57,59-60]
treprostinil Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.4 pKi 45,56
pKi 8.4 [45,56]
SQ-27986 Small molecule or natural product Hs Full agonist 8.0 pKi 40
pKi 8.0 (Ki 1x10-8 M) [40]
BW 245C Small molecule or natural product Rn Full agonist 7.8 pKi 60
pKi 7.8 [60]
PGD2 Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Mm Full agonist 7.7 pKi 24
pKi 7.7 [24]
PGD2 Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Rn Full agonist 7.6 pKi 60
pKi 7.6 [60]
RS 93520 Small molecule or natural product Hs Partial agonist 7.5 pKi 40
pKi 7.5 (Ki 3.16x10-8 M) [40]
L-888,291 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 pKi 12
pKi 7.4 [12]
PGE1 Small molecule or natural product Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 7.3 pKi 59
pKi 7.3 [59]
ZK118182 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.3 pKi 40
pKi 7.3 (Ki 5.01x10-8 M) [40]
carbacyclin Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 pKi 1
pKi 6.9 [1]
L-644,698 Small molecule or natural product Rn Full agonist 6.8 pKi 60
pKi 6.8 [60]
PGE2 Small molecule or natural product Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Immunopharmacology Ligand Hs Full agonist 6.5 – 7.0 pKi 1,5,59
pKi 6.5 – 7.0 [1,5,59]
15-deoxy-Δ12,14-PGJ2 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.6 pKi 59
pKi 6.6 [59]
BW 245C Small molecule or natural product Mm Full agonist 6.6 pKi 24
pKi 6.6 [24]
iloprost Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Full agonist 6.0 – 6.6 pKi 1,56,59
pKi 6.0 – 6.6 [1,56,59]
PGF Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Immunopharmacology Ligand Hs Full agonist 6.1 – 6.4 pKi 1,59
pKi 6.1 – 6.4 [1,59]
U46619 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Full agonist 5.4 – 5.9 pKi 1,59
pKi 5.4 – 5.9 [1,59]
butaprost (free acid form) Small molecule or natural product Click here for species-specific activity table Hs Full agonist 4.9 pKi 1
pKi 4.9 [1]
cloprostenol Small molecule or natural product Click here for species-specific activity table Hs Full agonist 4.8 pKi 1
pKi 4.8 [1]
View species-specific agonist tables
Agonist Comments
Reference [40] uses human platelet preparations instead of transfected cells.

BW 245C is a useful selective DP1 agonist [13,50,55].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
TG11-77 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 5.1 pKB 3
pKB 5.1 (KB 7.32x10-6 M) [3]
TG6-129 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 4.8 pKB 10
pKB 4.8 (KB 1.46x10-5 M) [10]
[3H]BWA868C Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.8 pKd 41
pKd 8.8 [41]
laropiprant Small molecule or natural product ? Antagonist 10.1 pKi 27,43
pKi 10.1 [27,43]
BWA868C Small molecule or natural product Hs Antagonist 8.6 – 9.3 pKi 5,13,59
pKi 8.6 – 9.3 [5,13,59]
S-5751 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.8 pKi 4
pKi 8.8 (Ki 1.58x10-9 M) [4]
ONO-AE3-237 Small molecule or natural product Hs Antagonist 7.7 pKi 17,48-49
pKi 7.7 [17,48-49]
BWA868C Small molecule or natural product Mm Antagonist 6.7 pKi 24
pKi 6.7 [24]
asapiprant Small molecule or natural product Immunopharmacology Ligand Hs Antagonist 6.6 pKi 26
pKi 6.6 (Ki 2.4x10-7 M) [26]
Description: Displacement of [3H]-PGD2 from DP receptor in human platelet membranes
AH6809 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 5.8 pKi 1
pKi 5.8 [1]
vidupiprant Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 8.4 pIC50 28
pIC50 8.4 (IC50 4x10-9 M) [28]
View species-specific antagonist tables
Antagonist Comments
References [4,41] use human platelet preparations instead of transfected cells.

BWA 868C [13,51] is a selective DP1 antagonist with pA2 of 7.8-9.5; S-5751 [4] has a lower selectivity.
Immunopharmacology Comments
DP1 receptor activation by prostaglandins mediates chemotaxis of pro-inflammatory cells such as basophils, eosinophils, and T cells. DP2 and DP1 may function to counteract each other's inflammatory action [18].
In human lung tissue specimens both DP1 and DP2 receptors are detected on alveolar macrophages, and activation of these two receptors aggravates airway neutrophilia in a mice model [20].
The DP1 has been identified as a new pathway controlling thymus atrophy and systemic T-cell pool (in a mouse model of acute lung injury) [52].
Immuno Process Associations
Immuno Process:  Inflammation
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gs family Adenylyl cyclase stimulation
References:  44
Tissue Distribution Click here for help
Eye: ciliary epithelial cells, longitudinal and circular ciliary muscles, retinal choroid, iris.
Species:  Human
Technique:  Radioligand binding.
References:  41
Eosinophils.
Species:  Human
Technique:  RT-PCR, Southern blotting and in situ hybridisation.
References:  11
Platelets.
Species:  Human
Technique:  Radioligand binding.
References:  41
Colon: mucous-secreting goblet cells.
Species:  Human
Technique:  in situ hybridisation.
References:  58
Brain leptomeninges.
Species:  Mouse
Technique:  In situ hybridization, Northern blot.
References:  36
Airway epithelium.
Species:  Mouse
Technique:  Immunohistochemistry.
References:  29
Arachnoid membrane.
Species:  Mouse
Technique:  Immunohistochemistry.
References:  30
Brain: choroid plexus, leptomeninges.
Spinal cord: ventral horn (motor neurons) > dorsal horn (sensory neurons) of the lumbar spinal cord.
Gastrointestinal tract: stomach, duodenum, ileum, colon (mucous-secreting goblet cells and cuboidal epithelium).
Species:  Rat
Technique:  in situ hybridisation.
References:  60
Expression Datasets Click here for help

Show »

Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

There should be a chart of expression data here, you may need to enable JavaScript!
Functional Assays Click here for help
Measurement of cAMP levels in HEK 293 cells transfected with the human DP receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Stimulation of cAMP accumulation.
References:  5,59-60
Measurement of cAMP levels in human platelets endogenously expressing the DP receptor.
Species:  Human
Tissue:  Platelets.
Response measured:  Stimulation of cAMP accumulation.
References:  38
Measurement of adenylate cyclase activity in human platelet membranes.
Species:  Human
Tissue:  Platelets.
Response measured:  Stimulation of AC activity.
References:  2,8,51
Measurement of Ca2+ levels in HEK 293 cells transfected with the human DP receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Increase in Ca2+ concentration.
References:  5
Measurement of cAMP accumulation 9n HEK 293 cells transfected with the rat DP receptor.
Species:  Rat
Tissue:  HEK 293 cells.
Response measured:  Stimulation of cAMP accumulation.
References:  60
Measurement of cAMP levels in human colonic adenocarcinoma cells, LS174T, endogenously expressing the DP receptor.
Species:  Human
Tissue:  LS174T cells.
Response measured:  Stimulation of cAMP accumulation.
References:  58
Measurement of mucin secretion in human colonic adenocarcinoma cells, LS174T, endogenously expressing the DP receptor.
Species:  Human
Tissue:  LS174T cells.
Response measured:  Stimulation of mucin secretion.
References:  58
Measurement of cAMP levels in a brain astrocytoma cell line transfected with the human DP receptor.
Species:  Human
Tissue:  Glial cells.
Response measured:  Stimulation of cAMP accumulation.
References:  56
Physiological Functions Click here for help
Inhibition of platelet aggregation.
Species:  Human
Tissue:  Whole blood.
References:  13,23,50
Inhibition of histamine release.
Species:  Rat
Tissue:  Peritoneal mast cells.
References:  6
Relaxation of the myometrium.
Species:  Human
Tissue:  Non-pregnant myometrium.
References:  9,39
Nasal blockage.
Species:  Human
Tissue:  In vivo.
References:  21
Relaxation of smooth muscle.
Species:  Human
Tissue:  Corpus cavernosum.
References:  31
Inhibition of superoxide release from neutrophils.
Species:  Human
Tissue:  Neutrophils.
References:  22
Inhibition of leukotriene B4 and superoxide anion (O2-) release from human neutrophils.
Species:  Human
Tissue:  Neutrophils.
References:  54
Regulation of eosinophil apoptosis.
Species:  Human
Tissue:  Eosinophils.
References:  58
Relaxation of pulmonary venous smooth muscle.
Species:  Human
Tissue:  Pulmonary venous preparations.
References:  53
Relaxation of bronchial smooth muscle.
Species:  Human
Tissue:  Bronchial preparations.
References:  34
Promoting endothelial barrier function via the cAMP/PKA/Tiam1/Rac1 pathway.
Species:  Mouse
Tissue:  Vascular endothelial cells
References:  25
Physiological Consequences of Altering Gene Expression Click here for help
DP receptor knockout OVA-challenged mice exhibit reduced Th2 cytokine levels and lymphocyte accumulation in the lung. In addition, they failed to produce asthmatic responses.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  29
DP receptor knockout mice exhibit reduced nicotinic acid-induced vasodilation.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  7
DP receptor knockout mice infected with Shistosomiasis display impaired retention of Langerhans cells in the epidermis.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  15
DP1 knockout mice do not display prostaglandin D2-induced sleep.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  30
DP1 deletion in mice augments aneurysm formation and the hypertensive response to Angiotensin II and accelerates atherogenesis and thrombogenesis.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  42
DP1 receptor deletion in mice augments intestinal tumour number in a mouse model of intestinal and colon cancer.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  47
DP1 receptor deletion in mice augments vascular leak and enhances tumour growth and vascularity in a mouse model of lung carcinoma.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  32
DP receptor knockout mice exhibit immature dermal mast cells and reduced response in passive cutaneous anaphylaxis, as observed in mice deficient in group III phospholipase A2.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  46
DP receptor knockout mice fail to show DP agonism-elicited resistance against croton oil-induced ear hyper permeability.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells
References:  25
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

Show »

Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Galctwi|Ptgdrtm1Sna Galctwi/Galctwi,Ptgdrtm1Sna/Ptgdrtm1Sna
B6.Cg-Galc Ptgdr
MGI:102966  MGI:95636  MP:0002182 abnormal astrocyte morphology PMID: 16624958 
Galctwi|Ptgdrtm1Sna Galctwi/Galctwi,Ptgdrtm1Sna/Ptgdrtm1Sna
B6.Cg-Galc Ptgdr
MGI:102966  MGI:95636  MP:0001393 ataxia PMID: 16624958 
Galctwi|Ptgdrtm1Sna Galctwi/Galctwi,Ptgdrtm1Sna/Ptgdrtm1Sna
B6.Cg-Galc Ptgdr
MGI:102966  MGI:95636  MP:0002083 premature death PMID: 16624958 
Ptgdrtm1Sna Ptgdrtm1Sna/Ptgdrtm1Sna
involves: 129P2/OlaHsd * C57BL/6
MGI:102966  MP:0002405 respiratory system inflammation PMID: 10720327 
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Asthma, susceptibility to, 1
Disease Ontology: DOID:2841
OMIM: 607277
Biologically Significant Variants Click here for help
Type:  Single nucleotide polymorphism
Species:  Human
Description:  TCTG haplotype (T-549C, C-441/T, T-197C and G+1044A) may be linked to an increased risk of post-coital pre-term birth.
References:  14
Type:  Single nucleotide polymorphism
Species:  Human
Description:  The 197T > C variant of the DP receptor may be linked to allergic asthma.
References:  33
Type:  Single nucleotide polymorphisms
Species:  Human
Description:  197T -> C, 441C -> T, and 549T -> C polymorphisms may be linked to asthma.
References:  35,37

References

Show »

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. Alvarez R, Eglen RM, Chang LF, Bruno JJ, Artis DR, Kluge AF, Whiting RL. (1991) Stimulation of prostaglandin D2 receptors on human platelets by analogs of prostacyclin. Prostaglandins, 42: 105-119. [PMID:1775633]

3. Amaradhi R, Banik A, Mohammed S, Patro V, Rojas A, Wang W, Motati DR, Dingledine R, Ganesh T. (2020) Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist for Use in Central Nervous System Disease Models. J Med Chem, 63 (3): 1032-1050. [PMID:31904232]

4. Arimura A, Yasui K, Kishino J, Asanuma F, Hasegawa H, Kakudo S, Ohtani M, Arita H. (2001) Prevention of allergic inflammation by a novel prostaglandin receptor antagonist, S-5751. J Pharmacol Exp Ther, 298 (2): 411-9. [PMID:11454901]

5. 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]

6. Chan CL, Jones RL, Lau HY. (2000) Characterization of prostanoid receptors mediating inhibition of histamine release from anti-IgE-activated rat peritoneal mast cells. Br J Pharmacol, 129 (3): 589-97. [PMID:10711359]

7. Cheng K, Wu TJ, Wu KK, Sturino C, Metters K, Gottesdiener K, Wright SD, Wang Z, O'Neill G, Lai E et al.. (2006) Antagonism of the prostaglandin D2 receptor 1 suppresses nicotinic acid-induced vasodilation in mice and humans. Proc Natl Acad Sci USA, 103 (17): 6682-7. [PMID:16617107]

8. Cooper B, Ahern D. (1979) Characterization of the platelet prostaglandin D2 receptor. Loss of prostaglandin D2 receptors in platelets of patients with myeloproliferative disorders. J Clin Invest, 64 (2): 586-90. [PMID:222813]

9. Fernandes B, Crankshaw D. (1995) Functional characterization of the prostanoid DP receptor in human myometrium. Eur J Pharmacol, 283 (1-3): 73-81. [PMID:7498323]

10. 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]

11. Gervais FG, Cruz RP, Chateauneuf A, Gale S, Sawyer N, Nantel F, Metters KM, O'neill GP. (2001) Selective modulation of chemokinesis, degranulation, and apoptosis in eosinophils through the PGD2 receptors CRTH2 and DP. J Allergy Clin Immunol, 108 (6): 982-8. [PMID:11742277]

12. Gervais FG, Morello JP, Beaulieu C, Sawyer N, Denis D, Greig G, Malebranche AD, O'Neill GP. (2005) Identification of a potent and selective synthetic agonist at the CRTH2 receptor. Mol Pharmacol, 67 (6): 1834-9. [PMID:15755909]

13. 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]

14. Grisaru-Granovsky S, Altarescu G, Finci S, Weintraub A, Tevet A, Samueloff A, Schimmel MS. (2010) Prostanoid DP receptor (PTGDR) variants in mothers with post-coital associated preterm births: preliminary observations. J Perinatol, 30 (1): 33-7. [PMID:19710676]

15. Hervé M, Angeli V, Pinzar E, Wintjens R, Faveeuw C, Narumiya S, Capron A, Urade Y, Capron M, Riveau G, Trottein F. (2003) Pivotal roles of the parasite PGD2 synthase and of the host D prostanoid receptor 1 in schistosome immune evasion. Eur J Immunol, 33: 2764-2772. [PMID:14515260]

16. Hirata M, Kakizuka A, Aizawa M, Ushikubi F, Narumiya S. (1994) Molecular characterization of a mouse prostaglandin D receptor and functional expression of the cloned gene. Proc Natl Acad Sci USA, 91 (23): 11192-6. [PMID:7972033]

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

18. Hohjoh H, Inazumi T, Tsuchiya S, Sugimoto Y. (2014) Prostanoid receptors and acute inflammation in skin. Biochimie, 107 Pt A: 78-81. [PMID:25179301]

19. Ishikawa TO, Tamai Y, Rochelle JM, Hirata M, Namba T, Sugimoto Y, Ichikawa A, Narumiya S, Taketo MM, Seldin MF. (1996) Mapping of the genes encoding mouse prostaglandin D, E, and F and prostacyclin receptors. Genomics, 32 (2): 285-8. [PMID:8833158]

20. Jandl K, Stacher E, Bálint Z, Sturm EM, Maric J, Peinhaupt M, Luschnig P, Aringer I, Fauland A, Konya V et al.. (2016) Activated prostaglandin D2 receptors on macrophages enhance neutrophil recruitment into the lung. J Allergy Clin Immunol, 137 (3): 833-43. [PMID:26792210]

21. Johnston SL, Smith S, Harrison J, Ritter W, Howarth PH. (1993) The effect of BAY u 3405, a thromboxane receptor antagonist, on prostaglandin D2-induced nasal blockage. J Allergy Clin Immunol, 91 (4): 903-9. [PMID:8473679]

22. Kanamori Y, Niwa M, Kohno K, Al-Essa LY, Matsuno H, Kozawa O, Uematsu T. (1997) Migration of neutrophils from blood to tissue: alteration of modulatory effects of prostanoid on superoxide generation in rabbits and humans. Life Sci, 60 (16): 1407-17. [PMID:9096262]

23. Keery RJ, Lumley P. (1988) AH6809, a prostaglandin DP-receptor blocking drug on human platelets. Br J Pharmacol, 94 (3): 745-54. [PMID:2460179]

24. Kiriyama M, Ushikubi F, Kobayashi T, Hirata M, Sugimoto Y, Narumiya S. (1997) Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol, 122 (2): 217-24. [PMID:9313928]

25. Kobayashi K, Tsubosaka Y, Hori M, Narumiya S, Ozaki H, Murata T. (2013) Prostaglandin D2-DP signaling promotes endothelial barrier function via the cAMP/PKA/Tiam1/Rac1 pathway. Arterioscler Thromb Vasc Biol, 33 (3): 565-71. [PMID:23307871]

26. Kugimiya A, Fujioka M, Tachibana Y, Murashi T. (2012) Sulfonamide derivative having PGD2 receptor antagonistic activity. Patent number: US8153793B2. Assignee: Shionogi and Co Ltd. Priority date: 27/09/2005. Publication date: 10/04/2012.

27. Lai E, Wenning LA, Crumley TM, De Lepeleire I, Liu F, de Hoon JN, Van Hecken A, Depré M, Hilliard D, Greenberg H et al.. (2008) Pharmacokinetics, pharmacodynamics, and safety of a prostaglandin D2 receptor antagonist. Clin Pharmacol Ther, 83 (6): 840-7. [PMID:17882161]

28. Liu J, Li AR, Wang Y, Johnson MG, Su Y, Shen W, Wang X, Lively S, Brown M, Lai S et al.. (2011) Discovery of AMG 853, a CRTH2 and DP Dual Antagonist. ACS Med Chem Lett, 2 (5): 326-30. [PMID:24900313]

29. Matsuoka T, Hirata M, Tanaka H, Takahashi Y, Murata T, Kabashima K, Sugimoto Y, Kobayashi T, Ushikubi F, Aze Y, Eguchi N, Urade Y, Yoshida N, Kimura K, Mizoguchi A, Honda Y, Nagai H, Narumiya S. (2000) Prostaglandin D2 as a mediator of allergic asthma. Science, 287: 2013-2017. [PMID:10720327]

30. Mizoguchi A, Eguchi N, Kimura K, Kiyohara Y, Qu WM, Huang ZL, Mochizuki T, Lazarus M, Kobayashi T, Kaneko T et al.. (2001) Dominant localization of prostaglandin D receptors on arachnoid trabecular cells in mouse basal forebrain and their involvement in the regulation of non-rapid eye movement sleep. Proc Natl Acad Sci USA, 98 (20): 11674-9. [PMID:11562489]

31. Moreland RB, Nehra A, Kim NN, Min KS, Albadawi H, Watkins MT, Goldstein I, Traish AM. (2002) Expression of functional prostaglandin D (DP) receptors in human corpus cavernosum smooth muscle. Int J Impot Res, 14 (6): 446-52. [PMID:12494276]

32. Murata T, Lin MI, Aritake K, Matsumoto S, Narumiya S, Ozaki H, Urade Y, Hori M, Sessa WC. (2008) Role of prostaglandin D2 receptor DP as a suppressor of tumor hyperpermeability and angiogenesis in vivo. Proc Natl Acad Sci USA, 105 (50): 20009-14. [PMID:19060214]

33. Noguchi E, Shibasaki M, Kamioka M, Yokouchi Y, Yamakawa-Kobayashi K, Hamaguchi H, Matsui A, Arinami T. (2002) New polymorphisms of haematopoietic prostaglandin D synthase and human prostanoid DP receptor genes. Clin Exp Allergy, 32 (1): 93-6. [PMID:12002745]

34. Norel X, Walch L, Labat C, Gascard JP, Dulmet E, Brink C. (1999) Prostanoid receptors involved in the relaxation of human bronchial preparations. Br J Pharmacol, 126 (4): 867-72. [PMID:10193766]

35. Oguma T, Palmer LJ, Birben E, Sonna LA, Asano K, Lilly CM. (2004) Role of prostanoid DP receptor variants in susceptibility to asthma. N Engl J Med, 351 (17): 1752-63. [PMID:15496624]

36. Oida H, Hirata M, Sugimoto Y, Ushikubi F, Ohishi H, Mizuno N, Ichikawa A, Narumiya S. (1997) Expression of messenger RNA for the prostaglandin D receptor in the leptomeninges of the mouse brain. FEBS Lett, 417 (1): 53-6. [PMID:9395073]

37. Sanz C, Isidoro-García M, Dávila I, Moreno E, Laffond E, Avila C, Lorente F. (2006) Promoter genetic variants of prostanoid DP receptor (PTGDR) gene in patients with asthma. Allergy, 61 (5): 543-8. [PMID:16629782]

38. Seiler S, Brassard CL, Federici ME. (1990) SQ-27986 inhibition of platelet aggregation is mediated through activation of platelet prostaglandin D2 receptors. Prostaglandins, 40: 119-130. [PMID:2171039]

39. Senior J, Sangha R, Baxter GS, Marshall K, Clayton JK. (1992) In vitro characterization of prostanoid FP-, DP-, IP- and TP-receptors on the non-pregnant human myometrium. Br J Pharmacol, 107 (1): 215-21. [PMID:1422574]

40. Sharif NA, Crider JY, Xu SX, Williams GW. (2000) Affinities, selectivities, potencies, and intrinsic activities of natural and synthetic prostanoids using endogenous receptors: focus on DP class prostanoids. J Pharmacol Exp Ther, 293 (2): 321-8. [PMID:10772998]

41. Sharif NA, Williams GW, Davis TL. (2000) Pharmacology and autoradiography of human DP prostanoid receptors using [(3)H]-BWA868C, a DP receptor-selective antagonist radioligand. Br J Pharmacol, 131 (6): 1025-38. [PMID:11082108]

42. Song WL, Stubbe J, Ricciotti E, Alamuddin N, Ibrahim S, Crichton I, Prempeh M, Lawson JA, Wilensky RL, Rasmussen LM et al.. (2012) Niacin and biosynthesis of PGD₂by platelet COX-1 in mice and humans. J Clin Invest, 122 (4): 1459-68. [PMID:22406532]

43. 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]

44. Sugimoto H, Shichijo M, Iino T, Manabe Y, Watanabe A, Shimazaki M, Gantner F, Bacon KB. (2003) An orally bioavailable small molecule antagonist of CRTH2, ramatroban (BAY u3405), inhibits prostaglandin D2-induced eosinophil migration in vitro. J Pharmacol Exp Ther, 305 (1): 347-52. [PMID:12649388]

45. 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]

46. Taketomi Y, Ueno N, Kojima T, Sato H, Murase R, Yamamoto K, Tanaka S, Sakanaka M, Nakamura M, Nishito Y et al.. (2013) Mast cell maturation is driven via a group III phospholipase A2-prostaglandin D2-DP1 receptor paracrine axis. Nat Immunol, 14 (6): 554-63. [PMID:23624557]

47. Tippin BL, Kwong AM, Inadomi MJ, Lee OJ, Park JM, Materi AM, Buslon VS, Lin AM, Kudo LC, Karsten SL et al.. (2014) Intestinal tumor suppression in ApcMin/+ mice by prostaglandin D2 receptor PTGDR. Cancer Med, 3 (4): 1041-51. [PMID:24729479]

48. 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]

49. 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]

50. Town MH, Dournaud P, Gu Y-Z, Schonbrunn A, Mazella J, Tannenbaum GS, Casals-Stenzel J, Schillinger E. (1983) Pharmacological and cardiovascular properties of a hydantoin derivative, BW245C, with high affinity and selectivity for PGD2 receptors. Prostaglandins, 25: 13-28. [PMID:6302737]

51. Trist DG, Collins BA, Wood J, Kelly MG, Robertson AD. (1989) The antagonism by BW A868C of PGD2 and BW245C activation of human platelet adenylate cyclase. Br J Pharmacol, 96 (2): 301-6. [PMID:2466517]

52. van den Brule S, Huaux F, Uwambayinema F, Ibouraadaten S, Yakoub Y, Palmai-Pallag M, Trottein F, Renauld JC, Lison D. (2014) Lung inflammation and thymic atrophy after bleomycin are controlled by the prostaglandin D2 receptor DP1. Am J Respir Cell Mol Biol, 50 (1): 212-22. [PMID:24003988]

53. Walch L, Labat C, Gascard JP, de Montpreville V, Brink C, Norel X. (1999) Prostanoid receptors involved in the relaxation of human pulmonary vessels. Br J Pharmacol, 126 (4): 859-66. [PMID:10193765]

54. Wheeldon A, Vardey CJ. (1993) Characterization of the inhibitory prostanoid receptors on human neutrophils. Br J Pharmacol, 108: 1051-1054. [PMID:8387383]

55. Whittle BJ, Moncada S, Mullane K, Vane JR. (1983) Platelet and cardiovascular activity of the hydantoin BW245C, a potent prostaglandin analogue. Prostaglandins, 25 (2): 205-23. [PMID:6344147]

56. 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]

57. 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]

58. Wright DH, Ford-Hutchinson AW, Chadee K, Metters KM. (2000) The human prostanoid DP receptor stimulates mucin secretion in LS174T cells. Br J Pharmacol, 131 (8): 1537-45. [PMID:11139429]

59. 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]

60. 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]

Contributors

Show »

How to cite this page