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. |
– |
– |