Product Type
All Products
New Products
Small Molecules
Peptides
Controlled Substances
Toxins
Caged Compounds
Fluorescent Probes
Screening Libraries
Ligand Sets
Other Product Types
Research Area
Cancer
Cardiovascular System
Endocrinology
Immunology
Neuroscience
Pain & Inflammation
Respiratory System
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.