Table 3.
Ion channel targets of cannabidiol
| Target | Concentration range (μM) | EC50/IC50 (μM) | Ki (μM) | Preparation or tissue | Assay type | Reference |
|---|---|---|---|---|---|---|
| Cav3.1 T-type | 10–2–10; (–) | 0.82 | ND | HEK293 cells/human | Patch clamp/ current clamp | [95] |
| Cav3.2 T-type | 10–2–10; (–) | 0.78 | ND | HEK293 cells/Hhuman | ||
| Cav3.3 T-type | 10–2–30; (–) | 3.7 | ND | HEK293 cells/human | ||
| TRPA1 | ND-100; (–) | 81.4 | ND | HEK 293 cells/rat | Calcium mobilization assays | [96] |
| 10–3–10; (–)* | 0.096 | ND | HEK 293 cells/rat | Calcium assay/Fluo4-AM | [97] | |
| 3–30; (+) | ND | ND | HEK 293 cells/rat | Patch clamp/current | [98] | |
| 10–3*–25; (–) | 0.11 | ND | HEK 293 cells/rat | Calcium assay/Fluo4-AM | [71] | |
| TRPM8 | 10–3–10; (–)* | 0.14 | ND | HEK 293 cells/rat | Calcium assay/Fluo4-AM | [97] |
| 10–3–25*; (–) | 0.06 | ND | HEK 293 cells/rat | [71] | ||
| TRPV1 | 0.1–10.0; (+) | 3.5 | ND | HEK 293 cells/human | Calcium assay/Fluo-3 | [19] |
| 10–3–25; (+)* | 1 | ND | HEK 293 cells/human | Calcium assay/Fluo4-AM | [71] | |
| ND-100; (NSC) | ND | ND | HEK 293 cells/rat | Calcium mobilization assays | [96] | |
| 3–30; (+) | ND | ND | HEK 293 cells/rat | Patch clamp/current | [98] | |
| 3; (NSC) | ND | ND | A549/human | Viability | [18] | |
| 3; (NSC) | ND | ND | A549/human | DNA fragmentation | ||
| 10–3–10; (+)* | 0.7* | ND | MDA-MB-231 cells | Calcium assay/Fluo4 | [99] | |
| TRPV2 | 0.05–103; (+)* | 31.7 | ND | HEK 293 cells/human | Calcium mobilization assay | [96] |
| 0.1–200.0; (+)* | 22.2 | ND | U87MG glioma cells/rat | Calcium mobilization assay | [100] | |
| 10–3–25*; (+) | 1.25 | ND | HEK 293 cells/rat | Calcium assay/Fluo4-AM | [71] | |
| 0.05–500.00; (+)* | 3.7 | ND | HEK 293 cells/rat | Calcium mobilization assay | [96] | |
| 3–30; (+) | ND | ND | HEK293 cells/rat | Patch clamp/current | [98] | |
| 3; (NSC) | ND | ND | H460/human | Viability | [18] | |
| 3; (NSC) | ND | ND | H460/human | DNA fragmentation | ||
| TRPV3 | 10–1–103; (+)* | 3.7 | ND | HEK 293 cells/rat | Calcium assay/Fluo4-AM | [101] |
| TRPV4 | 10–2–102; (+)* | 0.8 | ND | HEK 293 cells/rat | Calcium assay/Fluo4-AM | |
| VDAC1 | 20; (–) | ND | ND | Liver VDAC1 channel in planar lipid bilayer/sheep | Bilayer Clamp BC-525B amplifier/current | [84] |
| 0.1–75.0; (+)* | ND | Kd; 11.2 | Liver VDAC1 channel in planar lipid bilayer/sheep | Thermophoretic analysis/CBD–VDAC1 interaction |
TRP = transient receptor potential; TRPA1 = TRP ankyrin type 1; TRPM8 = TRP subfamily M; TRPV1 = TRP vanilloid-type 1; VDAC = voltage-dependent anion channel; NSC = no significant change; ND = not described; HEK = human embryonic kidney; CBD = cannabidiol; (+) = stimulation; (–): inhibition
*Estimated from plots in cited paper