Table 4.
Functionality of phytogenic, endogenous, and synthetic cannabinoid ligands at TRPV4.
| TRPV4 | |||||||
|---|---|---|---|---|---|---|---|
| Compound | Functionality | Efficacy* (μM) | Potency EC50 (μM) | Desensitization** (μM) | Cell type | References | |
| AEA | Agonist (Indirect activation) | - | - | - | TRPV4-HEK-293 | Watanabe et al. (2003) | |
| 2-AG | Agonist (Indirect activation) | - | - | - | TRPV4-HEK-293 | Watanabe et al. (2003) | |
| NTyr | Agonist | - | 55.59 ± 7.79 | - | TRPV4-HEK-293 | Raboune et al. (2014) | |
| NTrp | Agonist | - | 75.59 ± 7.79 | - | TRPV4-HEK-293 | Raboune et al. (2014) | |
| CBDV | Agonist | 30.2 ± 0.9 | 0.9 ± 0.1 | 2.9 ± 0.3 | TRPV4-HEK-293 | De Petrocellis et al. (2012a) | |
| THCV | Agonist | 59.8 ± 1.7 | 6.4 ± 0.7 | 3.2 ± 0.2 | TRPV4-HEK-293 | De Petrocellis et al. (2012a) | |
| CBG | Agonist | 23.7 ± 1.8 | 5.1 ± 1.6 | 1.3 ± 0.1 | TRPV4-HEK-293 | De Petrocellis et al. (2012a) | |
| CBGA | Agonist | 36.5 ± 1.9 | 28.8 ± 0.3 | 3.6 ± 0.3 | TRPV4-HEK-293 | De Petrocellis et al. (2012a) | |
| CBGV | Agonist | 26.1 ± 1.7 | 22.2 ± 3.7 | 1.8 ± 0.1 | TRPV4-HEK-293 | De Petrocellis et al. (2012a) | |
| CBN | Agonist | 15.3 ± 1.5 | 16.1 ± 4.5 | 5.4 ± 0.8 | TRPV4-HEK-293 | De Petrocellis et al. (2012a) | |
| SR141716A | - | <10 | NA | 2.0 ± 0.1 | TRPV4-HEK-293 | Soethoudt et al. (2017) | |
| SR144528 | - | <10 | NA | >100 | TRPV4-HEK-293 | Soethoudt et al. (2017) | |
| AM251 | - | <10 | NA | 1.2 ± 0.1 | TRPV4-HEK-293 | Soethoudt et al. (2017) | |
| Gp-1a | - | <10 | NA | 2.2 ± 0.1 | TRPV4-HEK-293 | Soethoudt et al. (2017) | |
| WIN55,212-2 | - | <10 | NA | 16.1 ± 1.7 | TRPV4-HEK-293 | Soethoudt et al. (2017) | |
| (R)-AM1241 | - | <10 | NA | 8.7 ± 0.5 | TRPV4-HEK-293 | Soethoudt et al. (2017) | |
| (S)-AM1241 | - | <10 | NA | 8.6 ± 0.3 | TRPV4-HEK-293 | Soethoudt et al. (2017) | |
| AM630 | - | <10 | NA | 3.2 ± 0.1 | TRPV4-HEK-293 | Soethoudt et al. (2017) | |
| HU308 | - | <10 | NA | >100 | TRPV4-HEK-293 | Soethoudt et al. (2017) | |
| HU910 | - | <10 | NA | >100 | TRPV4-HEK-293 | Soethoudt et al. (2017) | |
| JWH133 | - | 13.6 ± 0.8 | 12.0 ± 3.0 | >100 | TRPV4-HEK-293 | Soethoudt et al. (2017) | |
*Efficacy as % of ionomycin 4 μM. **Desensitization vs. standardized agonist (4-α-phorbol-12,13-didecanoate, 4αPDD) at EC50 concentrations. NA, No activity.