Nomenclature |
C3a receptor |
C5a1 receptor |
C5a2 receptor |
HGNC, UniProt |
C3AR1, Q16581
|
C5AR1, P21730
|
C5AR2, Q9P296
|
Principal transduction |
Gi/o, Gz
|
Gi/o, Gz, G16 (Buhl et al., 1993) |
– |
Rank order of potency |
C3a > C5a 653
|
C5a, C5a des-Arg (C5) > C3a 653
|
– |
Endogenous agonists (pKi) |
– |
RP-S19 (RPS19, P39019) 675
|
– |
Selective agonists (pKi) |
E7 (pEC50 8.7) 654
|
N-methyl-Phe-Lys-Pro-D-Cha-Cha-D-Arg-CO2H (pIC50 7.6) 664,666
|
– |
Selective antagonists (pKi) |
SB290157 (pIC50 7.6) 652
|
CHIPS (pKd 9.0) 670, W54011 (8.7) 672, AcPhe-Orn-Pro-D-Cha-Trp-Arg (pIC50 7.9) 674, N-methyl-Phe-Lys-Pro-D-Cha-Trp-D-Arg-CO2H (pIC50 7.2) 666
|
– |
Radioligands (Kd) |
[125I]C3a (human) (Agonist, Full agonist) (3.85x10-9 M) 657
|
[125I]C5a (human) (Agonist, Full agonist) (2x10-9 M) 661
|
[125I]C5a (human) (Agonist, Full agonist) |
Comment |
– |
– |
Binds C5a complement factor, but appears to lack G protein signalling and has been termed a decoy receptor 671
|