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. 2013 Dec 17;170(8):1459–1581. doi: 10.1111/bph.12445
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