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. 2015 Dec 9;172(24):5744–5869. doi: 10.1111/bph.13348
Nomenclature PAR1 PAR2 PAR3 PAR4
HGNC, UniProt F2R, P25116 F2RL1, P55085 F2RL2, O00254 F2RL3, Q96RI0
Agonist proteases thrombin (F2, P00734), activated protein C (PROC, P04070), matrix metalloproteinase 1 (MMP1, P45452), matrix metalloproteinase 13 (MMP13, P45452) [70] Trypsin, tryptase, TF/VIIa, Xa thrombin (F2, P00734) thrombin (F2, P00734), trypsin, cathepsin G (CTSG, P08311)
Selective agonists TFLLR‐NH2 (pEC50 5.4) [340] GB110 (pEC50 6.5) [98], 2‐furoyl‐LIGRLO‐amide (pK i 5.4) [1243], SLIGKV‐NH2 [1069], SLIGRL‐NH2 [1069] AYPGKF‐NH2, GYPGKF‐NH2, GYPGQV‐NH2
Selective antagonists vorapaxar (pK i 8.1) [281], atopaxar (pIC50 7.7) [978], RWJ‐56110 (pIC50 6.4) [48] GB88 (pIC50 5.7) [1813], P2pal18s [1705]
Labelled ligands [3H]haTRAP (Agonist) (pK d 7.8) [15] 2‐furoyl‐LIGRL[N‐(Alexa Fluor 594)‐O]‐NH2 (Agonist) [771], 2‐furoyl‐LIGRL[N[3H]propionyl]‐O‐NH2 (Agonist) [771], [3H]2‐furoyl‐LIGRL‐NH2 (Selective Agonist) [903], trans‐cinnamoyl‐LIGRLO [N‐[3H]propionyl]‐NH2 (Agonist) [28]
Comments TFLLR‐NH2 is selective relative to the PAR2 receptor [155, 915]. 2‐Furoyl‐LIGRLO‐NH2 activity was measured via calcium mobilisation in HEK 293 cells which constitutively coexpress human PAR1 and PAR2.