Therapeutic Targets Database
BIDD Pharmainformatics Databases


TTD Target ID: TTDS00170

Target Information
NameProstacyclin receptor    
Type of targetSuccessful target    
SynonymsIP prostanoid receptor    
PGI receptor    
Prostaglandin I2 receptor    
Prostanoid IP receptor    
DiseaseAnalgesics    [1]
Diabetes mellitus    [2]
Inflammatory pain    [1]
Drug(s)Dinoprost TromethamineApprovedAborting second-trimester pregnancy (between 12th to 18th week of gestation)[3][4]
EpoprostenolApprovedPulmonary hypertension[5][6][7]
MisoprostolApprovedMedical abortion[3][8][9]
TreprostinilApprovedPulmonary arterial hypertension[10]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
Vascular smooth muscle contraction
UniProt IDP43119
FunctionReceptor for prostacyclin (prostaglandin i2 or pgi2). The activity of this receptor is mediated by g(s) proteins which activate adenylate cyclase.    
Related US Patent6,417,186
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
AntagonistDinoprost Tromethamine[3][4]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The role of IP prostanoid receptors in inflammatory pain. Trends Pharmacol Sci. 1998 Apr;19(4):141-7. To Reference
Ref 2Reduced IP receptors in STZ-induced diabetic rat kidneys and high-glucose-treated mesangial cells. Am J Physiol Renal Physiol. 2004 Oct;287(4):F673-81. Epub 2004 May 25. To Reference
Ref 3Palmitoylation of the human prostacyclin receptor. Functional implications of palmitoylation and isoprenylation. J Biol Chem. 2003 Feb 28;278(9):6947-58. Epub 2002 Dec 17. To Reference
Ref 4Molecular cloning of human prostacyclin receptor cDNA and its gene expression in the cardiovascular system. Circulation. 1994 Oct;90(4):1643-7. To Reference
Ref 5Novel signaling pathways promote a paracrine wave of prostacyclin-induced vascular smooth muscle differentiation. J Mol Cell Cardiol. 2009 May;46(5):682-94. Epub 2009 Jan 23. To Reference
Ref 6Signaling through Gi family members in platelets. Redundancy and specificity in the regulation of adenylyl cyclase and other effectors. J Biol Chem. 2002 Nov 29;277(48):46035-42. Epub 2002 Sep 23. To Reference
Ref 7Expression of human hexosaminidase-A phenotype depends on genes assigned to chromosomes 5 and 15. Birth Defects Orig Artic Ser. 1976;12(7):192-6. To Reference
Ref 8The future potential of eicosanoids and their inhibitors in paediatric practice. Drugs. 1998 Aug;56(2):169-76. To Reference
Ref 9Structural organization and chromosomal assignment of the human prostacyclin receptor gene. Genomics. 1995 May 1;27(1):142-8. To Reference
Ref 10Dosing considerations in the use of intravenous prostanoids in pulmonary arterial hypertension: an experience-based review. Am Heart J. 2009 Apr;157(4):625-35. To Reference
Ref 11Bioorg. Med. Chem. Lett. 5(10):1071-1076 (1995) To Reference
Ref 12J Med Chem. 2010 Jan 14;53(1):18-36.Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor antagonist, as a novel antiplatelet agent that does not prolong bleeding. To Reference
Ref 13Bioorg Med Chem Lett. 2006 Sep 15;16(18):4861-4. Epub 2006 Jul 11.Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6. To Reference
Ref 14Bioorg Med Chem Lett. 2005 Jul 1;15(13):3279-83.Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2. To Reference
Ref 15J Med Chem. 2007 Feb 22;50(4):794-806.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). To Reference


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