Prostacyclin receptor

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Prostaglandin I2 (prostacyclin) receptor (IP)
Symbol(s) PTGIR; IP; MGC102830; PRIPR
External IDs OMIM: 600022 MGI99535 Homologene7496
RNA expression pattern


More reference expression data

Human Mouse
Entrez 5739 19222
Ensembl ENSG00000160013 ENSMUSG00000043017
Uniprot P43119 Q3U4F1
Refseq NM_000960 (mRNA)
NP_000951 (protein)
NM_008967 (mRNA)
NP_032993 (protein)
Location Chr 19: 51.82 - 51.82 Mb Chr 7: 16.07 - 16.07 Mb
Pubmed search [1] [2]

Prostacyclin receptor (or prostaglandin I2 receptor) is a receptor for prostacyclin.

It is a member of the G-protein coupled receptor family. Prostacyclin, the major product of cyclooxygenase in macrovascular endothelium, elicits a potent vasodilation and inhibition of platelet aggregation through binding to this receptor.[1]


When binding a prostacyclin-molecule, the receptor changes conformation and activates Gs, with its activation of cAMP and increase in protein kinase A (PKA) activity.

In vasodilation

In vasodilation, the PKA activity causes phosphorylation of MLCK, decreasing its activity, resulting in dephosphorylation of MLC of myosin. The smooth muscle relaxation leads to vasodilation.[2]


The receptor is encoded by the human gene PTGIR.[1]

See also


  1. 1.0 1.1 "Entrez Gene: PTGIR prostaglandin I2 (prostacyclin) receptor (IP)". 
  2. Walter F., PhD. Boron. Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. ISBN 1-4160-2328-3.  Page 479

Further reading

  • Coleman RA, Smith WL, Narumiya S (1994). "International Union of Pharmacology classification of prostanoid receptors: properties, distribution, and structure of the receptors and their subtypes.". Pharmacol. Rev. 46 (2): 205-29. PMID 7938166.
  • Rauvala H, Peng HB (1997). "HB-GAM (heparin-binding growth-associated molecule) and heparin-type glycans in the development and plasticity of neuron-target contacts.". Prog. Neurobiol. 52 (2): 127-44. PMID 9185236.
  • Smyth EM, FitzGerald GA (2003). "Human prostacyclin receptor.". Vitam. Horm. 65: 149-65. PMID 12481546.
  • Boie Y, Rushmore TH, Darmon-Goodwin A, et al. (1994). "Cloning and expression of a cDNA for the human prostanoid IP receptor.". J. Biol. Chem. 269 (16): 12173-8. PMID 7512962.
  • Katsuyama M, Sugimoto Y, Namba T, et al. (1994). "Cloning and expression of a cDNA for the human prostacyclin receptor.". FEBS Lett. 344 (1): 74-8. PMID 7514139.
  • Ogawa Y, Tanaka I, Inoue M, et al. (1995). "Structural organization and chromosomal assignment of the human prostacyclin receptor gene.". Genomics 27 (1): 142-8. PMID 7665161.
  • Duncan AM, Anderson LL, Funk CD, et al. (1995). "Chromosomal localization of the human prostanoid receptor gene family.". Genomics 25 (3): 740-2. PMID 7759114.
  • Nakagawa O, Tanaka I, Usui T, et al. (1994). "Molecular cloning of human prostacyclin receptor cDNA and its gene expression in the cardiovascular system.". Circulation 90 (4): 1643-7. PMID 7923647.
  • Bonaldo MF, Lennon G, Soares MB (1997). "Normalization and subtraction: two approaches to facilitate gene discovery.". Genome Res. 6 (9): 791-806. PMID 8889548.
  • Sasaki Y, Takahashi T, Tanaka I, et al. (1997). "Expression of prostacyclin receptor in human megakaryocytes.". Blood 90 (3): 1039-46. PMID 9242534.
  • Fisch A, Tobusch K, Veit K, et al. (1997). "Prostacyclin receptor desensitization is a reversible phenomenon in human platelets.". Circulation 96 (3): 756-60. PMID 9264479.
  • Smyth EM, Li WH, FitzGerald GA (1998). "Phosphorylation of the prostacyclin receptor during homologous desensitization. A critical role for protein kinase c.". J. Biol. Chem. 273 (36): 23258-66. PMID 9722557.
  • Kömhoff M, Lesener B, Nakao K, et al. (1999). "Localization of the prostacyclin receptor in human kidney.". Kidney Int. 54 (6): 1899-908. doi:10.1046/j.1523-1755.1998.00213.x. PMID 9853255.
  • Hayes JS, Lawler OA, Walsh MT, Kinsella BT (1999). "The prostacyclin receptor is isoprenylated. Isoprenylation is required for efficient receptor-effector coupling.". J. Biol. Chem. 274 (34): 23707-18. PMID 10446129.
  • Smyth EM, Austin SC, Reilly MP, FitzGerald GA (2000). "Internalization and sequestration of the human prostacyclin receptor.". J. Biol. Chem. 275 (41): 32037-45. doi:10.1074/jbc.M003873200. PMID 10889200.
  • Lawler OA, Miggin SM, Kinsella BT (2001). "Protein kinase A-mediated phosphorylation of serine 357 of the mouse prostacyclin receptor regulates its coupling to G(s)-, to G(i)-, and to G(q)-coupled effector signaling.". J. Biol. Chem. 276 (36): 33596-607. doi:10.1074/jbc.M104434200. PMID 11443126.
  • Zhang Z, Austin SC, Smyth EM (2001). "Glycosylation of the human prostacyclin receptor: role in ligand binding and signal transduction.". Mol. Pharmacol. 60 (3): 480-7. PMID 11502878.
  • Fortier I, Patry C, Lora M, et al. (2001). "Immunohistochemical localization of the prostacyclin receptor (IP) human bone.". Prostaglandins Leukot. Essent. Fatty Acids 65 (2): 79-83. doi:10.1054/plef.2001.0292. PMID 11545623.

Template:Membrane-protein-stub This article incorporates text from the United States National Library of Medicine, which is in the public domain.