Table 1.
Affinity and efficacy of CBD at molecular targets in the ‘expanded endocannabinoid system,’ data pooled from Supporting Information Appendix S2
| Target | Assaya | Pooled means, number of studiesb |
|---|---|---|
| CB2 receptor | A: versus [3H]CP55,940 binding; human CB2 transfected cell cultures, or rat RBL-2H3 leukemia cells, centrifuged membranes | Ki = 3612 ± 1382 nM, n = 6 |
| CB2 receptor | E: [35S]GTPγS binding; human CB2-CHO cells | EMAX = −15% below basal at 10 μM EC50 = 503 ± 2080 nM; n = 1 |
| CB2 receptor | E: antagonism of CP55,940-induced [35S]GTPγS binding; human CB2-CHO cells | KB = 65 ± 54.1 nM, n = 1 |
| GPR55 | E: antagonism of agonist-induced signalling; human cell cultures or CB2-CHO cells | IC50 = 433 ± 42.6 nM, n = 3 |
| TRPV1 channels | A: versus [3H]-resiniferatoxin binding; human TRPV1-HEK293 cell membranes | Ki = 3600 ± 200 (SD) nM, n = 1 |
| TRPV1 channels | E: [Ca2+]i elevation in human TRPV1-HEK293 cells | EMAX 53.4 ± 5.03%; n = 4 EC50 = 1900 ± 802 nM |
| TRPA1 channels | E: [Ca2+]i elevation in rat TRPA1-HEK293 cell membranes | EMAX 98.6 ± 10.39% EC50 = 100 ± 10 nM; n = 3 |
| TRPV2 channels | E: [Ca2+]i elevation in rat or human TRPV2-HEK293 cell membranes | EMAX 100.2 ± 34.50% EC50 = 12.2 ± 9.77 μM; n = 3 |
| TRPM8 channels | E: [Ca2+]i elevation in rat TRPM8-HEK293 cell membranes | Signals as functional antagonist EC50 = 70.0 ± 14.1 nM; n = 2 |
aA, affinity; E, efficacy. Other abbreviations as defined in the manuscript.
bNumber of studies that met the CV-Cochrane ‘skew test’ (see Supporting Information Appendix S2).