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. 2018 Oct 6;11(4):100. doi: 10.3390/ph11040100

Table 1.

Ligands of itch-related TRP channels.

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]