Nomenclature |
FPR1 |
FPR2/ALX |
FPR3 |
HGNC, UniProt |
FPR1, P21462
|
FPR2, P25090
|
FPR3, P25089
|
Principal transduction |
Gi/o, Gz
|
Gi
778
|
– |
Rank order of potency |
fMet-Leu-Phe > cathepsin G (CTSG, P08311) > annexin I 776,783
|
LXA4=aspirin triggered lipoxin A4=ATLa2>LTC4=LTD4>>15-deoxy-LXA4>>fMet-Leu-Phe 765,766,768,770,784
|
– |
Selective agonists (pKi) |
fMet-Leu-Phe (pEC50 10.1–10.2) 769,782
|
– |
– |
Endogenous antagonists (pKi) |
spinorphin (Selective) (pIC50 4.3) 777,780
|
aspirin triggered lipoxin A4 (Selective), LXA4 (Selective) (pEC50 ∼12.0) 775, resolvin D1 (Selective) (pEC50 ∼11.9) 775
|
– |
Endogenous agonists(pKi) |
F2L (HEBP1, Q9NRV9) (Selective) (pEC50 8.0–8.2) 779
|
– |
– |
Selective antagonists (pKi) |
cyclosporin H (6.1–7.1) 785,786, t-Boc-FLFLF (6.0–6.5) 785
|
ATLa2 771
|
– |
Radioligands (Kd) |
[3H]fMet-Leu-Phe (Agonist, Full agonist) (5×10−10–2.51×10−8 M) 774
|
[3H]LXA4 (Agonist, Full agonist) (5×10−10–7×10−10 M) 766,767
|
– |
Comment |
A FITC-conjugated fMLP analogue has been used for binding to the mouse recombinant receptor 773
|
The agonist activity of the lipid mediators described has been questioned 772,781, which may derive from batch-to-batch differences, partial agonism or biased agonism |
– |