Table 1.
Effect of the compounds on Ca2+ mobilization in FPR1/FPR2 transfected cells, human and mouse neutrophils
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|---|---|---|---|---|---|
| Compound | FPR1 | FPR2 | Human PMN (w/o probenecid) |
Human PMN (with probenecid) |
Mouse PMN |
| EC50, µM (Efficacy, %) | |||||
| (S)-9a | 0.43 ± 0.13 (130) |
0.096 ± 0.027 (120) |
0.064 ± 0.026 (100) |
0.060 ± 0.021 (105) |
0.24 ± 0.07 (110) |
| (R)-9a | N.A. | 0.23 ± 0.083 (100) |
0.92 ± 0.28 (40) |
0.88 ± 0.25 (95) |
4.9 ± 1.4 (30) |
| (S)-9b | N.A. | 1.6 ± 0.36 (115) |
12.6 ± 3.7 (55) |
0.66 ± 0.18 (130) |
1.7 ± 0.44 (50) |
| (R)-9b | N.A. | N.A. | N.A. | N.A. | 2.3 ± 0.73 (65) |
| (S)-9c | N.A. | N.A. | N.A. | N.A. | 2.5 ± 0.61 (60) |
| (R)-9c | N.A. | 0.26 ± 0.064 (65) |
N.A. | 0.97 ± 0.34 (40) |
3.8 ± 1.3 (35) |
| (S)-9d | N.A. | 0.73 ± 0.23 (75) |
1.8 ± 0.42 (30) |
0.27 ± 0.082 (105) |
3.9 ± 1.5 (75) |
| (R)-9d | N.A. | N.A. | N.A. | N.A. | 2.1 ± 0.58 (80) |
| (S)-9e | 0.95 ± 0.26 (115) |
0.43 ± 0.11 (135) |
1.8 ± 0.37 (85) |
0.45 ± 0.13 (120) |
2.8 ± 0.64 (80) |
| (R)-9e | N.A. | 0.31 ± 0.092 (90) |
0.62 ± 0.24 (40) |
0.49 ± 0.16 (115) |
1.0 ± 0.27 (55) |
| (S)-9f | N.A. | 0.86 ± 0.21 (40) |
N.A. | 1.1 ± 0.36 (55) |
2.3 ± 0.35 (25) |
| (R)-9f | N.A. | N.A. | N.A. | N.A. | 2.5 ± 0.42 (25) |
