Proteinase-Activated Receptor (PAR) Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
PAR1 Human F2R NM_001992 P25116
Mouse F2r NM_010169 P30558
Rat F2r NM_012950 P26824
PAR2 Human F2RL1 NM_005242 P55085
Mouse F2rl1 NM_007974 P55086
Rat F2rl1 NM_053897 Q63645
PAR3 Human F2rl2 NM_004101 O00254
Mouse F2rl2 NM_010170 O08675
Rat F2rl2 NM_053313 Q920E1
PAR4 Human F2rl3 NM_003950 Q96RI0
Mouse F2rl3 NM_007975 O88634
Rat F2rl3 NM_053808 Q920E0

Proteinase-Activated Receptor Pharmacological Data

Receptor Subtype PAR1 PAR2 PAR3 PAR4
Transduction Mechanism Gq/11 (↑IP3/DAG)
Gi
G12/13
Gq/11 (↑IP3/DAG)
Gi
Not Known Gq/11 (↑IP3/DAG)
Agonist Protease Thrombin Trypsin Thrombin Thrombin/Trypsin
Primary Distribution Platelets, endothelium, vascular smooth muscle, Gl tract epithelium, leukocytes, fibroblasts, neurons, mast cells Endothelium, leukocytes, Gl tract epithelium, airway and vascular smooth muscle, neurons, mast cells, renal tubular cells Airway smooth muscle, platelets Platelets, megakaryocytes
Likely Physiological Roles Platelet activation, pro-inflammatory, embryonic development, regulation of vascular tone Pro-inflammatory, mediates nociceptin, airway protection, regulation of vascular tone Cofactor for PAR4 Platelet activation
Selective Agonists TFLLR-NH2 (1464)
(EC50 = 1.9 μM)
SLIGRL-NH2 (1468)
(EC50 ~ 5 μM)
SLIGKV-NH2 (3010)
(IC50 = 10.4 μM)
- AY-NH2 (AYPGKF-NH2) (1487)
(EC50 = 15 μM)
Selective Antagonists SCH 79797 (1592)
(EC50 = 70 nM)
- - tcY-NH2 (trans-cinnamoyl-YPGKF-NH2) (1488)

References

Hollenberg and Compton (2002) International Union of Pharmacology. XXVIII. Proteinase-activated receptors. Pharmacol.Rev. 54 203. de Garavilla et al (2001) Agonists of proteinase-activated receptor 1 induce plasma extravasation by a neurogenic mechanism. Br.J.Pharmacol. 133 975. Nystedt et al (1994) Molecular cloning of a potential proteinase activated receptor. Proc.Natl.Acad.Sci.USA 91 9208. Hollenberg and Saifeddine (2001) Proteinase-activated receptor 4 (PAR4): activation and inhibition of rat platelet aggregation by PAR4-derived peptides. Can.J.Physiol.Pharmacol. 79 439. Ahn et al (2000) Inhibition of cellular action of thrombin by N3-cyclopropyl-7-{[4-(1-methylethyl)phenyl]methyl}-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine (SCH79797), a nonpeptide thrombin receptor antagonist. Biochem.Pharmacol. 60 1425.