Table 1.
Ligands | Targets | Potencies | References |
---|---|---|---|
HC-030031 | TRPA1 | IC50 = 6.2 and 5.3 μM for AITC- and formalin-evoked Ca2+ influx, respectively. | [129] |
A-967079 | TRPA1 | IC50 = 0.3 μM for mTRPA1 | [130] |
AP18 | TRPA1 | IC50 = 3.1 μM and 4.5 μM for hTRPA1 and mTRPA1, respectively | [131] |
AM-0902 | TRPA1 | IC50 = 24 nM for hTRPA1 | [132] |
AMG9810 | TRPV1 | IC50 = 24.5 nM for hTRPV1 | [133] |
SB366791 | TRPV1 | IC50 = 5.7 nM and 7.5 nM for hTRPV1 and rTRPV1, respectively | [134] |
PAC-14028 | TRPV1 | IC50 = 55.0 nM for rTRPV1 | [135] |
SB-705498 | TRPV1 | IC50 = 3 nM for capsaicin-induced activation of hTRPV1 | [136] |
17R-RvD1 | TRPV3 | IC50 = 398 nM for hTRPV3 | [137] |
HC-067047 | TRPV4 | IC50 = 48 nM, 133 nM, and 17 nM for hTRPV4, rTRPV4, and mTRPV4, respectively | [138] |
GSK2193874 | TRPV4 | IC50 = 40 nM and 2 nM for hTRPV4 and rTRPV4, respectively | [139] |
ML204 | TRPC4 TRPC5 TRPC6 |
IC50 = 0.96 μM for mTRPC4β and about 65% inhibition of TRPC5 and 38% inhibition of TRPC6 at 10 μM | [140] |
HC-070 | TRPC4 TRPC5 |
IC50 = 46.0 nM for hTRPC4 IC50 = 9.3 nM for hTRPC5 |
[141] |
1,8-cineole | TRPM8 TRPA1 |
EC50 = 3.4 mM for TRPM8 IC50 = 3.4 mM for TRPA1 |
[142,143] |
M8-Ag | TRPM8 TRPA1 |
EC50 = 45 nM for TRPM8 EC50 > 4 μM for TRPA1 |
[144] |
WS-12 | TRPM8 | EC50 = 193 nM for hTRPM8 | [145,146] |