PAR1 | Proteinase-activated receptors | IUPHAR/BPS Guide to PHARMACOLOGY

PAR1

Target id: 347

Nomenclature: PAR1

Family: Proteinase-activated receptors

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     PAR1 has curated GtoImmuPdb data

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 425 5q13 F2R coagulation factor II thrombin receptor
Mouse 7 430 13 D1 F2r coagulation factor II (thrombin) receptor
Rat 7 432 2q12 F2r coagulation factor II (thrombin) receptor
Previous and Unofficial Names
protease-activated receptor 1 | coagulation factor II (thrombin) receptor
Database Links
Specialist databases
GPCRDB par1_human (Hs), par1_mouse (Mm), par1_rat (Rn)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human protease-activated receptor 1 (PAR1) bound with antagonist vorapaxar at 2.2 angstrom
PDB Id:  3VW7
Ligand:  vorapaxar
Resolution:  2.2Å
Species:  Human
References:  33
Natural/Endogenous Ligands
thrombin {Sp: Human} , thrombin {Sp: Mouse} , thrombin {Sp: Rat}
Agonist proteases (Human)
thrombin (F2, P00734), activated protein C (PROC, P04070), matrix metalloproteinase 1 (MMP1, P45452), matrix metalloproteinase 13 (MMP13, P45452)  [8]

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]haTRAP Hs Agonist 7.8 pKd 1
pKd 7.8 (Kd 1.5x10-8 M) [1]
TFLLR-NH2 Hs Full agonist 5.4 pEC50 13
pEC50 5.4 (EC50 3.9x10-6 M) [13]
F16357 Hs Agonist 5.2 pIC50
pIC50 5.2 (IC50 6.4x10-6 M)
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
vorapaxar Hs Antagonist 8.1 pKi 11
pKi 8.1 (Ki 8.1x10-9 M) [11]
RWJ-56110 Hs Antagonist 6.4 pIC50 4
pIC50 6.4 (IC50 4.4x10-7 M) [4]
Immunopharmacology Comments
PAR1 has been found to mediate the effects of neutrophil elastase (NE) on γδ T cell activation, as the PAR1 inhibitor RWJ-56110 abrogates NE (from neutrophils)-induced activation of these T cells [28]. We have therefore included PAR1 in the GtoImmuPdb.
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 2 GO processes
GO:0002248 connective tissue replacement involved in inflammatory response wound healing IDA
GO:0006954 inflammatory response ISS
Immuno Process:  Tissue repair
GO Annotations:  Associated to 1 GO processes
GO:0002248 connective tissue replacement involved in inflammatory response wound healing IDA
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 3 GO processes
GO:0032651 regulation of interleukin-1 beta production ISS
GO:2000484 positive regulation of interleukin-8 secretion IDA
GO:2000778 positive regulation of interleukin-6 secretion IDA
Expression Datasets

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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]

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Physiological Consequences of Altering Gene Expression
PAR1-deficiency reduces neurological deficits, endothelial barrier leakage and neuronal degeneration. Decreased infarction, vascular disruption and protection and against T2 lesions, brain haemorrhage and raised interleukin 1β levels.
Species:  Mouse
Tissue:  Brain, neurons, astrocytes
Technique:  Gene knock-outs
References:  12,14-15,18,22,29-30
PAR1-deficiency reduces bone to tissue volume ratio
Species:  Mouse
Tissue:  Bone
Technique:  Gene knock-outs
References:  6
PAR1-deficiency enhances fear and impairs learning and memory via modulation of neuronal and synaptic plasticity. PAR1 deficient mice show impairments of long-term potentiation, deficits in hippocampal memory and enhancement of fear after conditioning.
Species:  Mouse
Tissue:  Brain
Technique:  Gene knock-outs
References:  2-3,9
PAR1-deficiency prevents kallikrein 6 mediated neurodegeneration. PAR1 knockout mice show reduced KlK6 activation, reduced neurotoxic effects of KlK6, and protection against Klk6-mediated oligodendrogliopathy.
Species:  Mouse
Tissue:  Brain, motorneurons
Technique:  Gene knock-outs
References:  10,27
PAR1 contributes to innate immune response during viral infection. PAR1 knockout mice have higher viral loads in both CVB3-induced myocarditis and influenza A infection.
Species:  Mouse
Tissue:  Cardiac, pulmonary
Technique:  Gene knock-outs
References:  5
PAR1 contributes to glioma-induced brain edema. PAR1 knockout mice had decreased levels of H. pylori after infection, protects host against severe Helicobacter-induced gastritis.
Species:  Mouse
Tissue:  Brain
Technique:  Gene knock-outs
References:  32
PAR1 impairs host defence in pneumococcal pneumonia. PAR1 knockout mice had better survival and lower bacterial loads after infection with S. pneumonia.
Species:  Mouse
Tissue:  Pulmonary
Technique:  Gene knock-outs
References:  24
PAR1 down-regulates the inflammatory and humoral response to Helicobacter pylori. PAR1 knockout mice had decreased levels of H. pylori after infection, protects host against severe Helicobacter-induced gastritis.
Species:  Mouse
Tissue:  Epithelial cells
Technique:  Gene knock-outs
References:  31
Absence of PAR1 protects against fMLP-induced goblet cell metaplasia
Species:  Mouse
Tissue:  Pulmonary
Technique:  Gene knock-outs
References:  7
PAR1 helps regulate nicotine reward. PAR1 knockout mice have diminished nicotine-induced conditioned place-preference and dopamine release.
Species:  Mouse
Tissue:  Dopaminergic neurons
Technique:  Gene knock-outs
References:  19-20
PAR1-deficiency reduces liver fibrosis. PAR1 knockout mice showed decreased incidence of fibrosis and T-lymphocyte infiltration following carbon tetrachloride-induced toxicity.
Species:  Mouse
Tissue:  Liver
Technique:  Gene knock-outs
References:  23
PAR1-deficiency is protective against renal ischemia reperfusion injury. PAR1 knockout mice were protected from renal failure, had reduced mortality, tubular injury, neutrophil accumulation and lower chemokine levels.
Species:  Mouse
Tissue:  Kidney
Technique:  Gene knock-outs
References:  25
PAR1 knockout mice show protection against bleomycin-induced acute lung injury, inflammation and fibrosis.
Species:  Human
Tissue:  Lung
Technique:  Gene knock-outs
References:  16-17
Xenobiotics Influencing Gene Expression
Baicalin (PubChem CID 64982) down-regulates PAR1 mRNA and PAR1 expression in rats with focal cerebral ischemic reperfusion injury.
Species:  Rat
Tissue:  Brain
Technique:  IP infusion
References:  34
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd * C57BL/6
MGI:101802  MP:0010695 abnormal blood pressure regulation PMID: 8972001 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd * C57BL/6
MGI:101802  MP:0004883 abnormal blood vessel healing PMID: 10591683 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
involves: 129S4/SvJae * C57BL/6J
MGI:101802  MP:0001544 abnormal cardiovascular system physiology PMID: 8632823 
F2rtm2Cgh F2rtm2Cgh/F2rtm2Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MP:0001544 abnormal cardiovascular system physiology PMID: 20152175 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd * C57BL/6
MGI:101802  MP:0004181 abnormal carotid artery morphology PMID: 10591683 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
involves: 129S4/SvJae * C57BL/6J
MGI:101802  MP:0005621 abnormal cell physiology PMID: 8632823 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
B6.Cg-F2r
MGI:101802  MP:0005621 abnormal cell physiology PMID: 11850418 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd
MGI:101802  MP:0008713 abnormal cytokine level PMID: 18305483 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd * C57BL/6
MGI:101802  MP:0002161 abnormal fertility/fecundity PMID: 8972001 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
involves: 129S4/SvJae * C57BL/6
MGI:101802  MP:0005085 abnormal gallbladder physiology PMID: 17431214 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
B6.129P2-F2r
MGI:101802  MP:0003921 abnormal heart left ventricle morphology PMID: 17967980 
F2rtm1Pago|F3tm1.1Dwr F2rtm1Pago/F2rtm1Pago,F3tm1.1Dwr/F3tm1.1Dwr
B6.129-F3 F2r
MGI:101802  MGI:88381  MP:0009660 abnormal induced retinal neovascularization PMID: 17363687 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd * C57BL/6
MGI:101802  MP:0010155 abnormal intestine physiology PMID: 15345469 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd
MGI:101802  MP:0002339 abnormal lymph node morphology PMID: 18305483 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
B6.Cg-F2r
MGI:101802  MP:0003202 abnormal neuron apoptosis PMID: 14980205 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
involves: 129S4/SvJae * C57BL/6J
MGI:101802  MP:0001712 abnormal placenta development PMID: 8632823 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
B6.Cg-F2r
MGI:101802  MP:0003228 abnormal sinus venosus PMID: 11533492 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd * C57BL/6
MGI:101802  MP:0000230 abnormal systemic arterial blood pressure PMID: 9918574 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd * C57BL/6
MGI:101802  MP:0010697 abnormal systemic arterial blood pressure regulation PMID: 8972001 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
B6.Cg-F2r
MGI:101802  MP:0003229 abnormal vitelline vasculature morphology PMID: 11533492 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
B6.Cg-F2r
MGI:101802  MP:0001719 absent vitelline blood vessels PMID: 11533492 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
B6.129P2-F2r
MGI:101802  MP:0000343 altered response to myocardial infarction PMID: 17967980 
F2rtm2Cgh F2rtm2Cgh/F2rtm2Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MP:0003051 curly tail PMID: 20152175 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
involves: 129S4/SvJae * C57BL/6J
MGI:101802  MP:0001698 decreased embryo size PMID: 8632823 
F2rtm1Ajc|F5tm1Dgi F2rtm1Ajc/F2rtm1Ajc,F5tm1Dgi/F5tm1Dgi
B6.Cg-F5 F2r
MGI:101802  MGI:88382  MP:0001698 decreased embryo size PMID: 11533492 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd * C57BL/6
MGI:101802  MP:0001876 decreased inflammatory response PMID: 17623652 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd
MGI:101802  MP:0009764 decreased sensitivity to induced morbidity/mortality PMID: 18305483 
F2rtm1Ajc|F2rl1tm1Cgh F2rtm1Ajc/F2rtm1Ajc,F2rl1tm1Cgh/F2rl1tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MGI:101910  MP:0008770 decreased survivor rate PMID: 16434493 
F2rtm2Cgh F2rtm2Cgh/F2rtm2Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MP:0008770 decreased survivor rate PMID: 20152175 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd
MGI:101802  MP:0008734 decreased susceptibility to endotoxin shock PMID: 18305483 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd * C57BL/6
MGI:101802  MP:0008539 decreased susceptibility to induced colitis PMID: 15545995 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd * C57BL/6
MGI:101802  MP:0003071 decreased vascular permeability PMID: 11120874 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
B6.Cg-F2r
MGI:101802  MP:0000292 distended pericardium PMID: 11533492 
F2rtm2Cgh F2rtm2Cgh/F2rtm2Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MP:0001785 edema PMID: 20152175 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
involves: 129S4/SvJae * C57BL/6J
MGI:101802  MP:0003984 embryonic growth retardation PMID: 8632823 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
B6.Cg-F2r
MGI:101802  MP:0003984 embryonic growth retardation PMID: 11533492 
F2rtm1Ajc|F2rl1tm1Cgh F2rtm1Ajc/F2rtm1Ajc,F2rl1tm1Cgh/F2rl1tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MGI:101910  MP:0008762 embryonic lethality PMID: 16434493 
F2rtm1Ajc|F2rl1tm1Cgh|F2rl3tm1Cgh F2rtm1Ajc/F2rtm1Ajc,F2rl1tm1Cgh/F2rl1tm1Cgh,F2rl3tm1Cgh/F2rl3tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MGI:101910  MGI:1298207  MP:0008762 embryonic lethality PMID: 16434493 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd * C57BL/6
MGI:101802  MP:0006207 embryonic lethality during organogenesis PMID: 8972001 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
involves: 129S4/SvJae * C57BL/6J
MGI:101802  MP:0006207 embryonic lethality during organogenesis PMID: 8632823 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
B6.Cg-F2r
MGI:101802  MP:0006207 embryonic lethality during organogenesis PMID: 11533492 
F2rtm1Ajc|F5tm1Dgi F2rtm1Ajc/F2rtm1Ajc,F5tm1Dgi/F5tm1Dgi
B6.Cg-F5 F2r
MGI:101802  MGI:88382  MP:0006207 embryonic lethality during organogenesis PMID: 11533492 
F2rtm1Pago F2rtm1Pago/F2rtm1Pago
involves: 129P2/OlaHsd
MGI:101802  MP:0008466 enlarged mesenteric lymph nodes PMID: 18305483 
F2r/F2rl1tm1.1Cgh F2r/F2rl1tm1.1Cgh/F2r/F2rl1tm1.1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MP:0000914 exencephaly PMID: 20152175 
F2rtm2Cgh F2rtm2Cgh/F2rtm2Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MP:0000914 exencephaly PMID: 20152175 
F2rtm1.1Cgh|F2rl1tm2Cgh|Tg(Tek-F2r)1Cgh F2rtm1.1Cgh/F2rtm1.1Cgh,F2rl1tm2Cgh/F2rl1tm2Cgh,Tg(Tek-F2r)1Cgh/0
involves: 129S4/SvJae * C57BL/6
MGI:101802  MGI:101910  MGI:4438038  MP:0000914 exencephaly PMID: 20152175 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
B6.Cg-F2r
MGI:101802  MP:0005244 hemopericardium PMID: 11533492 
F2rtm1Ajc|F5tm1Dgi F2rtm1Ajc/F2rtm1Ajc,F5tm1Dgi/F5tm1Dgi
B6.Cg-F5 F2r
MGI:101802  MGI:88382  MP:0005244 hemopericardium PMID: 11533492 
F2rtm1Ajc F2rtm1Ajc/F2rtm1Ajc
B6.Cg-F2r
MGI:101802  MP:0001914 hemorrhage PMID: 11533492 
F2rtm1Ajc|F5tm1Dgi F2rtm1Ajc/F2rtm1Ajc,F5tm1Dgi/F5tm1Dgi
B6.Cg-F5 F2r
MGI:101802  MGI:88382  MP:0001914 hemorrhage PMID: 11533492 
F2r+|F2rtm2Cgh|F2rl1+|F2rl1tm2Cgh F2rtm2Cgh/F2r+,F2rl1tm2Cgh/F2rl1+
involves: 129S4/SvJae * C57BL/6
MGI:101802  MGI:101910  MP:0000928 incomplete cephalic closure PMID: 20152175 
F2rtm1Pago|Tg(MMTV-PyVT)634Mul F2rtm1Pago/F2rtm1Pago,Tg(MMTV-PyVT)634Mul/0
B6.Cg-F2r Tg(MMTV-PyVT)634Mul
MGI:101802  MGI:2679594  MP:0010383 increased adenoma incidence PMID: 18757438 
F2rtm1Ajc|F2rl1tm1Cgh F2rtm1Ajc/F2rtm1Ajc,F2rl1tm1Cgh/F2rl1tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MGI:101910  MP:0009763 increased sensitivity to induced morbidity/mortality PMID: 16434493 
F2rtm1Ajc|F2rl1tm1Cgh F2rtm1Ajc/F2rtm1Ajc,F2rl1tm1Cgh/F2rl1tm1Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MGI:101910  MP:0008735 increased susceptibility to endotoxin shock PMID: 16434493 
F2rtm2Cgh F2rtm2Cgh/F2rtm2Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MP:0006208 lethality throughout fetal growth and development PMID: 20152175 
F2rtm1Pago|Tg(MMTV-PyVT)634Mul F2rtm1Pago/F2rtm1Pago,Tg(MMTV-PyVT)634Mul/0
B6.Cg-F2r Tg(MMTV-PyVT)634Mul
MGI:101802  MGI:2679594  MP:0001883 mammary adenocarcinoma PMID: 18757438 
F2rtm1Ajc|F5tm1Dgi F2rtm1Ajc/F2rtm1Ajc,F5tm1Dgi/F5tm1Dgi
B6.Cg-F5 F2r
MGI:101802  MGI:88382  MP:0005312 pericardial effusion PMID: 11533492 
F2rtm2Cgh F2rtm2Cgh/F2rtm2Cgh
involves: 129S4/SvJae * C57BL/6
MGI:101802  MP:0003054 spina bifida PMID: 20152175 
Biologically Significant Variants
Type:  Intervening sequence-14 A/T dimorphism
Species:  Human
Description:  Increased platelet aggregation and procoagulant responses were observed with PAR1 IVSn-14 A allele homozygotes
References:  21,26

References

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1. Ahn HS, Foster C, Boykow G, Arik L, Smith-Torhan A, Hesk D, Chatterjee M. (1997) Binding of a thrombin receptor tethered ligand analogue to human platelet thrombin receptor. Mol. Pharmacol., 51 (2): 350-6. [PMID:9203642]

2. Almonte AG, Hamill CE, Chhatwal JP, Wingo TS, Barber JA, Lyuboslavsky PN, David Sweatt J, Ressler KJ, White DA, Traynelis SF. (2007) Learning and memory deficits in mice lacking protease activated receptor-1. Neurobiol Learn Mem, 88 (3): 295-304. [PMID:17544303]

3. Almonte AG, Qadri LH, Sultan FA, Watson JA, Mount DJ, Rumbaugh G, Sweatt JD. (2013) Protease-activated receptor-1 modulates hippocampal memory formation and synaptic plasticity. J. Neurochem., 124 (1): 109-22. [PMID:23113835]

4. Andrade-Gordon P, Maryanoff BE, Derian CK, Zhang HC, Addo MF, Darrow AL, Eckardt AJ, Hoekstra WJ, McComsey DF, Oksenberg D et al.. (1999) Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. Proc. Natl. Acad. Sci. U.S.A., 96 (22): 12257-62. [PMID:10535908]

5. Antoniak S, Owens 3rd AP, Baunacke M, Williams JC, Lee RD, Weithäuser A, Sheridan PA, Malz R, Luyendyk JP, Esserman DA et al.. (2013) PAR-1 contributes to the innate immune response during viral infection. J. Clin. Invest., 123 (3): 1310-22. [PMID:23391721]

6. Aronovich A, Nur Y, Shezen E, Rosen C, Zlotnikov Klionsky Y, Milman I, Yarimi L, Hagin D, Rechavi G, Martinowitz U et al.. (2013) A novel role for factor VIII and thrombin/PAR1 in regulating hematopoiesis and its interplay with the bone structure. Blood, 122 (15): 2562-71. [PMID:23982175]

7. Atzori L, Lucattelli M, Scotton CJ, Laurent GJ, Bartalesi B, De Cunto G, Lunghi B, Chambers RC, Lungarella G. (2009) Absence of proteinase-activated receptor-1 signaling in mice confers protection from fMLP-induced goblet cell metaplasia. Am. J. Respir. Cell Mol. Biol., 41 (6): 680-7. [PMID:19307611]

8. Austin KM, Covic L, Kuliopulos A. (2013) Matrix metalloproteases and PAR1 activation. Blood, 121 (3): 431-9. [PMID:23086754]

9. Bourgognon JM, Schiavon E, Salah-Uddin H, Skrzypiec AE, Attwood BK, Shah RS, Patel SG, Mucha M, John Challiss RA, Forsythe ID et al.. (2013) Regulation of neuronal plasticity and fear by a dynamic change in PAR1-G protein coupling in the amygdala. Mol. Psychiatry, 18 (10): 1136-45. [PMID:23032873]

10. Burda JE, Radulovic M, Yoon H, Scarisbrick IA. (2013) Critical role for PAR1 in kallikrein 6-mediated oligodendrogliopathy. Glia, 61 (9): 1456-70. [PMID:23832758]

11. Chackalamannil S, Wang Y, Greenlee WJ, Hu Z, Xia Y, Ahn HS, Boykow G, Hsieh Y, Palamanda J, Agans-Fantuzzi J et al.. (2008) Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity. J. Med. Chem., 51 (11): 3061-4. [PMID:18447380]

12. Cheng Y, Xi G, Jin H, Keep RF, Feng J, Hua Y. (2014) Thrombin-induced cerebral hemorrhage: role of protease-activated receptor-1. Transl Stroke Res, 5 (4): 472-5. [PMID:24323711]

13. Chung AW, Jurasz P, Hollenberg MD, Radomski MW. (2002) Mechanisms of action of proteinase-activated receptor agonists on human platelets. Br. J. Pharmacol., 135 (5): 1123-32. [PMID:11877318]

14. Guo H, Liu D, Gelbard H, Cheng T, Insalaco R, Fernández JA, Griffin JH, Zlokovic BV. (2004) Activated protein C prevents neuronal apoptosis via protease activated receptors 1 and 3. Neuron, 41 (4): 563-72. [PMID:14980205]

15. Hamill CE, Mannaioni G, Lyuboslavsky P, Sastre AA, Traynelis SF. (2009) Protease-activated receptor 1-dependent neuronal damage involves NMDA receptor function. Exp. Neurol., 217 (1): 136-46. [PMID:19416668]

16. Howell DC, Johns RH, Lasky JA, Shan B, Scotton CJ, Laurent GJ, Chambers RC. (2005) Absence of proteinase-activated receptor-1 signaling affords protection from bleomycin-induced lung inflammation and fibrosis. Am. J. Pathol., 166 (5): 1353-65. [PMID:15855637]

17. Jenkins RG, Su X, Su G, Scotton CJ, Camerer E, Laurent GJ, Davis GE, Chambers RC, Matthay MA, Sheppard D. (2006) Ligation of protease-activated receptor 1 enhances alpha(v)beta6 integrin-dependent TGF-beta activation and promotes acute lung injury. J. Clin. Invest., 116 (6): 1606-14. [PMID:16710477]

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Nigel Bunnett, Kathryn DeFea, Justin Hamilton, Morley D. Hollenberg, Rithwik Ramachandran, JoAnn Trejo.
Proteinase-activated receptors: PAR1. Last modified on 01/02/2018. Accessed on 18/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=347.