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. t-Boc, N-tert-butoxycarbonyl group; i-Boc, iso-butoxycarbonyl group. pIC50 is defined as the negative logarithm of the IC50; same for pKi. N/D, binding affinity or potency was not determined.
| 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) |
| Cyclosporin H | Binding | pKi = 7.00 | FPR1 | (Wenzel-Seifert et al., 1991) |
| Cyclosporin A | 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) |
| Chenodeoxycholic acid (CDCA) | Binding | pKi = 4.76 – 4.52 | FPR1 > FPR2/ALX | (Chen et al., 2000) |
| Deoxycholic acid (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) |