Previously reported GPCR ligands that induced Ca2+ mobilization in human neutrophils and FPR-transfected HL-60 cells
The EC50 values are presented as the mean ± S.D. of three independent experiments, in which median effective concentration values (EC50) were determined by nonlinear regression analysis of the dose-response curves (five to six points) generated using GraphPad Prism 5 with 95% confidence interval (P < 0.05). Efficacy is expressed as percentage of the response induced by 5 nM fMLF (FPR1) or 5 nM WKYMVm (FPR2 and FPR3).
| Compound | Previously Reported Activity for GPCR | Ca2+ Mobilization, EC50, and Efficacy | |||
|---|---|---|---|---|---|
| Neutrophils | FPR1 | FPR2 | FPR3 | ||
| μM (%) | |||||
| PD168368 | BB1 antagonist | 0.91 ± 0.34 (70) | 0.57 ± 0.17 (95) | 0.24 ± 0.08 (90) | 2.7 ± 0.4 (60) |
| PD176252 | BB1/BB2 antagonist | 0.72 ± 0.21 (75) | 0.31 ± 0.09 (100) | 0.66 ± 0.12 (95) | N.A. |
| A-71623 | CCK-1 receptor agonist | 18.3 ± 3.1 (55) | 18.0 ± 3.8 (50) | 16.4 ± 3.1 (85) | N.A. |
N.A., nonactive compound (cell activation was <30% of control level over a concentration range of 0–40 μM).