Table 2. Data summary for TRPV4 antagonists (a).
Antagonist |
Potency
(IC50, μM) |
Species | Cross-reactivity |
---|---|---|---|
RN-1734 | 2.3 5.9 3.2 |
human mouse rat |
--- |
RN-9893 | <0.12 <0.06 <0.12 |
human mouse rat |
--- |
HC-067047 | 0.048 0.017 0.133 |
human mouse rat |
inhibits TRPM8, HERG at submicromolar |
Ruthenium Red | <0.086-1 <0.21-1 <0.2-0.33 |
human mouse rat |
inhibits all TRPVs, TRPM6, TRPM8, TRPA1, RyR1-3 |
Capsazepine | 18.6 13.5 |
human rat |
Inhibits TRPV1, TRPM8 |
Citral | 32 | mouse | Inhibits TRPA1, activates TRPV1, TRPV3, TRPM8 |