TABLE 6.
Antagonists for the human formyl peptide receptors
Antagonists for the FPRs are listed in the order of their approximate potency, except that antagonists of same types are listed together.
| Ligand | Assay | Potency | Selectivity | References |
|---|---|---|---|---|
| Chemotaxis inhibitory protein of S. aureus (CHIPS) | Binding | pKd = 7.46 | FPR1 | Haas et al. (2004) |
| FPRL1-inhibitor protein (FLIPr) | Binding, Ca2+ flux | N.D. | FPR2/ALX ≫ FPR1 | Prat et al. (2006) |
| Trp-Arg-Trp-Trp-Trp-Trp (WRW4) | Ca2+ flux | pIC50 = 6.64 | FPR2/ALX ≫ FPR1 ≈ FPR3 | Bae et al. (2004) |
| CsH | Binding | pKi = 7.00 | FPR1 | Wenzel-Seifert et al. (1991) |
| CsA | Enzyme release | pKi = 6.22 | FPR1 | Yan et al. (2006) |
| i-Boc-Met-Leu-Phe | O2− generation | pIC50 = 6.60 | FPR1 | Derian et al. (1996) |
| t-Boc-Met-Leu-Phe | Enzyme release | pIC50 = 6.19 | FPR1 | Freer et al. (1980) |
| t-Boc-Phe-Leu-Phe-Leu-Phe | Enzyme release | pIC50 = 6.59 | FPR1 ≫ FPR2/ALX | Freer et al. (1980) |
| Quin-C7 | Binding | pKi = 5.19 | FPR2/ALX | Zhou et al. (2007) |
| CDCA | Binding | pKi = 4.76–4.52 | FPR1 > FPR2/ALX | Chen et al. (2000) |
| DCA | Binding | pKi = 4.00 | FPR1 | Chen et al. (2002) |
| Spinorphin | O2− generation | pIC50 = 4.30 | FPR1 | Yamamoto et al. (1997); Liang et al. (2000) |
t-Boc, N-tert-butoxycarbonyl group; i-Boc, -butoxycarbonyl group; pIC50, negative logarithm of the IC50; pKi, negative logarithm of Ki; N.D., binding affinity or potency was not determined.