Table 1.
CB1/CB2 receptor-independent effects of endocannabinoids or analogs on potassium channels
| Cannabinoids | Channel targets | Changes in channel function | Cell models |
IC50/EC50 (Concentration range)a |
Ref | |
|---|---|---|---|---|---|---|
| AEA/methAEA (indirect) | BKCa | ↑ | HEK293 & Mouse aortic myocytes | (0.3–3.0 μM) | [36] | |
| AEA | BKCa | ↑ | EA.hy926 human endothelial-derived cell line | 1.1 μM | [37] | |
| NAGly | BKCa | ↑ | Endothelial cells & Isolated mouse aorta | (0.1–30 μM) | [38] | |
| AEA (extracellular)2-AGmethAEA | (h)CardiacKv4.3/KChIP2(≅ Ito, fast) | ↓↓↓ | CHO & Human right atrial appendage myocytes | 0.4 μM0.3 μM0.6 μM | [42] | |
| AEA | Ito | ↓ | Rat ventricular myocytes | (1–100 nM) | [44] | |
| 2-AGb | IA | ↓ | Mouse midbrain dopaminergic neurons | (0.03–30 μM) | [47] | |
| AEA (either side ofmembrane) | Kv3.1 (non-inactivating) | ↓ (into IA-type) | Xenopus oocytes &Rat hippocampal slices | (3 μM)(0.1–1 μM) | [61] | |
| AEA (extracellular) | Kv1.2 | ↓ | Murine fibroblasts(B82 cell line) | 2.7 μM | [48] | |
| AEA (extracellular)methAEA | Delayed rectifier Kv | ↓ | Rat aortic vascular smooth myocytes | 0.6 μM (10 μM) | [50] | |
| AEA (extracellular)2-AGmethAEA | Delayed rectifier Kv | ↓ | Rat primary cortical astrocytes & Neocortical slices | ~0.3 μM (1 μM) (1 μM) | [51] | |
| 2-AG | Delayed rectifier Kv | ↓ | Mouse insulinoma R7T1 β-cells | 20 μM | [54] | |
| AEA (extracellular) & 2-AG | hKv1.5 ISUS APD |
↓ ↓↑ |
Mouse fibroblastsHuman atrial cellsMouse left atria | 0.9–2.5 μM | [59] | |
| AEA (cytoplasmic) (as open channel blocker) | hKv1.5 | ↓ | HEK293 | 0.2 μM | [60] | |
| 2-AG (cytoplasmic) | KATP | ↓ | Mouse insulinoma R7T1 β-cells | 1 μM | [54] | |
| AEA | KATP (cromakalin-induced) | ↓ | Follicle-enclosed Xenopus oocytes | 8.1 μM | [29] | |
| AEAc (CB2 receptor-dependent) | KATP | ↑ | Rat ventricular myocytes | (1–100 nM) | [44] | |
| AEA/methAEAmethAEA | TASK-1 IKso |
↓ ↓ |
COS-7, CHO & HEK293Cerebellar neurons | 0.7 μM(10 μM) | [66] | |
aNumbers in parentheses denote the range of concentrations examined.
bThis effect was measured at 37°C (in contrast to room temperature at which the recording experiment to determine the endocannabinoid effect was conducted in other studies listed in this table).
cThis effect is CB2 receptor-dependent.