Table 3.
Summary of the effects of TRPV1 antagonists displaying differential effects on CGRP release elicited by maximally effective concentrations of capsaicin or PDBu
| Compound | Inhibition of 300 nM capsaicin response | Inhibition of 1 μM PDBu response | Reference | ||||
|---|---|---|---|---|---|---|---|
| pIC50 ± SEM | Inhibition (%) | n | pIC50 ± SEM | Inhibition (%) | n | ||
| ABT-102 | 7.62 ± 0.05 | 104 ± 4 | 3 | 8.18 ± 0.1** | 60 ± 2** | 2 | (Surowy et al., 2008) |
| AMG-8562 | 8.45 ± 0.08 | 100 ± 4 | 3 | 9.00 ± 0.18 | 19 ± 15** | 3 | (Lehto et al., 2008) |
| AMG-8563 | 8.27 ± 0.05 | 104 ± 3 | 3 | 8.90 ± 0.08** | 67 ± 2** | 3 | (Lehto et al., 2008) |
| Capsazepine | 6.15 ± 0.06 | 108 ± 5 | 3–6 | >4 | 0 | 3–6 | (Bevan et al., 2005) |
| SB366791 | ∼5 | ∼50% @ 10μM | 4 | >4 | 0 | 3 | (Gunthorpe et al., 2004) |
| HPPB | 5.76 ± 0.08 | 86 ± 9 | 3 | 6.34 ± 0.17 (EC50) | 162 ± 9 (Efficacy) | 2–3 | See methods |
**
P < 0.01, *P < 0.05.