Table I.
Major Receptor Targets of CBD and their Potential Indications in Brain Disorders
| Receptors | Ki (µM) | EC50/ IC50 (µM) | CBD activity | Potential indications [39, 48] | References |
|---|---|---|---|---|---|
| CB1 | 2.01 | > 30 | Negative allosteric modulator | Pain, cardiovascular diseases | [21–23, 40] |
| CB2 | ND | > 30 | Negative allosteric modulator | Pain | [22, 24] |
| GPR3 | ND | 1 | Inverse agonist | Neuropathic pain, neurodegenerative diseases | [30] |
| GPR6 | ND | 0.1 | Inverse agonist | Neuropathic pain, neurodegenerative diseases | [30] |
| GPR12 | ND | 10 | Inverse agonist | Neuropathic pain, neurodegenerative diseases | [29, 30] |
| GPR55 | ND | 0.445 | Antagonist | Epilepsy, neurodegenerative diseases | [22, 31, 32] |
| TRPM8 | ND | 0.06 – 0.14 | Antagonist | Pain | [27, 33] |
| TRPA1 | ND | 0.096 – 0.11 | Agonist | Pain, inflammation | [27, 33] |
| TRPV1 | ND | 1 – 3.5 | Agonist | Epilepsy, pain, inflammation, neurodegenerative diseases, psychosis | [27, 34] |
| TRPV2 | ND | 1.25 – 31.7 | Agonist | Epilepsy, pain, inflammation | [27, 35, 36] |
| 5-HT1A | 16 | ND | Agonist | Epilepsy, movement disorders, depression, anxiety, psychosis | [37, 38] |
| μ-opioid | 31.6 | 10 | Positive allosteric modulator | Neurodegenerative diseases, addiction | [40] |
| δ-opioid | 18.4 | 10.7 | Positive allosteric modulator | Neurodegenerative diseases, addiction | [40] |
| PPAR-γ | ND | 20.1 | Agonist | Neurodegenerative diseases, inflammation | [42, 43] |
| α1-glycine | ND | 12.3 | Positive allosteric modulator | Neurodegenerative diseases, inflammation | [44] |
| 132.4 | Agonist | ||||
| α1β-glycine | ND | 18.1 | Positive allosteric modulator | Neurodegenerative diseases, inflammation | [44] |
| 144.3 | Agonist | ||||
| α3-glycine | ND | 3 | Agonist | Neuropathic pain, inflammation | [45] |
| GABAA | ND | 0.9 – 23.1 | Positive allosteric modulator | Epilepsy, anxiety, insomnia | [47] |
| FAAH | ND | 15.2 – 27.5 | Inhibitor | Epilepsy, psychosis, insomnia | [27, 34] |
Abbreviations: 5-HT1A, Serotonin receptor 1A; CB, Cannabinoid receptor; FAAH, Fatty acid amide hydrolase; GABAA, γ-aminobutyric acid type A receptor; GPR, G protein-coupled receptor; ND, not determined; PPAR-γ, Peroxisome proliferator-activated receptor gamma; TRPA1, TRP channel of ankyrin type 1; TRPM8, TRP channel of melastatin type-8; TRPV1, TRP channel of vanilloid type-1; TRPV2, TRP channel of vanilloid type-2