C5a receptor affinity and antagonist activity of HC-[OP(D-Cha)WR] and AcF-[OP(D-Cha)WR]
Assay | AcF-[OP(D-Cha)WR] | HC-[OP(D-Cha)WR] | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| n | -log IC50 ± S.E. | IC50 | n | -log IC50 ± S.E. | IC50 | |||||
| Human PBMC receptor binding | 3 | 6.38 ± 0.34 | 417 nM | 3 | 6.50 ± 0.09 | 319 nM | ||||
|
n
| pKb ± S.E. |
K
b
|
n
| pKb ± S.E. |
K
b
| |||||
| Human PBMC β-Hex release | 4 | 8.60 ± 0.26 | 2.6 nM | 3 | 8.67 ± 0.24 | 2.15 nM | ||||
| Human PMN MPO release | 3 | 8.24 ± 0.18 | 5.82 nM | 3 | 9.03 ± 0.44 | 0.93 nM | ||||
β-Hex, β-hexosminidase; MPO, pyeloperoxidase.