Table 1.
A selection of receptors, ion channels, enzymes and cellular uptake processes that CBD has been reported to activate, antagonize or inhibit in vitro
| CBD concentration | Pharmacological target and effect | Reference |
|---|---|---|
| Receptors and channels | ||
| <1 µm | CB1 receptor (−) | [40] |
| CB2 receptor (−) | [40] | |
| GPR55 (−) | [41]† | |
| 5-HT3A ligand-gated channel (−)* | [42] | |
| TRPM8 cation channel (−) | [36] | |
| TRPA1 cation channel (+) | [36] | |
| 1–10 µm | PPARγ nuclear receptor (+) | [41]† |
| CaV3 T-type Ca2+ channels (−) | [43] | |
| TRPV1 cation channel (+) | [36] | |
| TRPV2 cation channel (+) | [36] | |
| >10 µm | 5-HT1A receptor (+) | [44]† |
| µ and δ opioid receptors (−)* | [44]† | |
| α1 and α1β glycine ligand-gated channels (+)* | [45] | |
| Enzymes | ||
| <1 µm | CYP1A1 (−) | [46] |
| 1–10 µm | CYP1A2 & CYP1B1 (−) | [46] |
| CYP2B6 (−) | [47] | |
| CYP2D6 (−) | [48] | |
| CYP3A5 (−) | [49] | |
| Mg2+-ATPase (−) | [44]† | |
| Arylalkylamine N-acetyltransferase (−) | [50] | |
| Indoleamine-2,3-dioxygenase (−) | [51] | |
| 15-lipoxygenase (−) | [52] | |
| Phospholipase A2 (+) | [44]† | |
| Glutathione peroxidase (+) | [13, 53] | |
| Glutathione reductase (+) | [13, 53] | |
| >10 µm | CYP2A6 (−) | [47] |
| CYP3A4 and CYP3A7 (−) | [49] | |
| Fatty acid amide hydrolase (−) | [36] | |
| 5-lipoxygenase (−) | [52] | |
| Superoxide dismutase (−) | [53] | |
| Catalase (−) | [53] | |
| NAD(P)H-quinone reductase (−) | [53] | |
| Progesterone 17α-hydroxylase (−) | [54, 55] | |
| Testosterone 6β-hydroxylase (−) | [54] | |
| Testosterone 16α-hydroxylase (−) | [54] | |
| Transporters and cellular uptake | ||
| <1 µm | Adenosine uptake by cultured microglia and macrophages (−) | [44]† |
| Calcium uptake by synaptosomes (−) | [44]† | |
| 1–10 µm | NE, DA, 5-HT and GABA uptake by synaptosomes (−) | [44]† |
| Anandamide and palmitoylethanolamide cellular uptake (−) | [36] | |
| P-glycoprotein (drug efflux transporter) (−) | [56] | |
| >10 µm | Choline uptake by rat hippocampal homogenates (−) | [44]† |
5-HT, 5-hydroxytryptamine; DA, dopamine; GABA, γ-aminobutyric acid; NE, norepinephrine.
*
Apparent allosteric modulation; (+). activation; (−), inhibition or antagonism.
†
Review article.