Name | In Vitro: IC50 for Different Activation Modes | In Vivo: Effect on Deep Tb | ||||
---|---|---|---|---|---|---|
CAP (500 nM) | pH (5.0) | Heat (45°C) | Dose | Route | Effect | |
nM | nM | nM | mg/kg | |||
A-425619 | 10 ± 2a | 13 ± 2a | 58 ± 4a | 4–100 | p.o. | ↑ab |
A-889425 | 335c | — | — | 4–13 | p.o. | ↑c |
2 | i.v. | ↑c | ||||
ABT-102 | 1d | 16d | 100d | 1–10 | p.o. | ↑e |
AMG0347 | 0.7 ± 0.1f | 0.8 ± 0.3f | 0.2 ± 0.1f | 0.01–0.5 | i.v. | ↑f |
AMG1629 | 0.6 ± 0.4a | 1 ± 0a | 0.2 ± 0.0a | 3 | p.o. | ↑a |
AMG2820 | 1 ± 0a | >4000a | 23 ± 6a | 3 | i.v. | ↑a |
AMG3731 | 6 ± 5a | 7 ± 1a | 5 ± 0a | 3–10 | p.o. | ↑a |
AMG 517 | 1 ± 1g | 0.5 ± 0.2g | 2 ± 1g | 0.1–3 | p.o. | ↑gh |
0.9 ± 0.8h | 0.5 ± 0.2h | — | 0.1 | i.v. | ↑i | |
AMG7988 | 14 ± 2a | >4000a | 360 ± 97a | 3 | i.v. | ↑a |
AMG8163 | 0.6 ± 0.3aj | 0.6 ± 0.3aj | 0.2 ± 0.1aj | 0.1–10 | p.o. | ↑ag |
0.3 | i.v. | ↑j | ||||
AMG8563 | 3 ± 1j | >4000j | 2 ± 0j | 3 | i.v. | ↑j |
AMG9810 | 79 ± 9a | 349 ± 66a | 9 ± 1a | 30 | i.p. | ↑a |
86 ± 39k | 294 ± 192k | 21 ± 17k | ||||
BCTC | 0.4 ± 0.3a | 0.5 ± 0.6a | 0.1 ± 0.0a | 3 | i.v. | ↑a |
0.5 ± 0.1k | 0.7 ± 0.4k | 0.6 ± 0.2k | ||||
Comp. 41 | 102 ± 12l | 16 ± 4l | — | 30 | p.o. | ↑l |
Comp. G | 1 ± 0a | 1 ± 0a | 2 ± 0a | 30 | p.o. | ↑a |
Comp. H | 18 ± 3a | 70 ± 5a | 16 ± 9a | 30 | p.o. | ↑a |
AMG7905 | 39 ± 17j | N.A. | N.A. | 0.3–30 | p.o. | ↓j |
AMG8562 | 2 ± 1j | N.A. | >4000j | 1–30 | p.o. | ↓j |
3 | i.v. | ↓j | ||||
JYL 1421 | 8a | N.A. | >4000j | 3–100 | p.o. | ↕a |
37m | — | — | 1–10 | i.p. | ↕m |
N.A., not applicable (IC50 for the marked activation mode could not have been measured, because potentiation was observed instead of inhibition); —, IC50 for this mode of activation was not determined; ↑, an increase in deep Tb; ↓, a decrease in deep Tb; ↕, no effect.
↵a Gavva et al. (2007b). pH of 5.5 was used in this study of A-425619 in which no TRPV1 inhibition occurred at pH of 5.0.
↵b Mills et al. (2008).
↵c McGaraughty et al. (2009). CAP concentration used in this study was not specified.
↵d Surowy et al. (2008). CAP concentration of 1 μM, pH of 5.5, and temperature of 50°C were used in this study.
↵e Honore et al. (2009).
↵f Steiner et al. (2007).
↵g Gavva et al. (2007a).
↵h Tamayo et al. (2008).
↵i Gavva et al. (2008).
↵j Lehto et al. (2008).
↵k Gavva et al. (2005b).
↵l Swanson et al. (2005). CAP concentration of 100 nM and a pH range of 5.8 to 6.0 were used in this study.
↵t Suh et al. (2003).