Table 4.
The binding affinities of the tested cannabinoids with FABP1. Ligand binding was determined via DAUDA displacement assay. The Kd value was determined from the COPASI fit of the ternary binding model to the DAUDA displacement data while EC50 and Emin were determined from fit of a three parameter dose response curve to the data. All parameter estimates are reported as means ± standard deviation from three replicate experiments performed on separate days. The ligands tested included THC, 11-OH-THC, cannabidiol (CBD) and the endogenous cannabinoids anandamide (AEA) and 2-arachidonoylglycerol (2AG).
| Kd (μM) | EC50 (μM) | Emin (% fluorescence remaining) | |
|---|---|---|---|
| THC | 0.30 ± 0.34 | 0.22 ± 0.13 | 52 ± 4.0 |
| 11-OH-THC | 0.86 ± 0.15 | 1.5 ± 0.23 | 23 ± 3.8 |
| CBD | 0.57 ± 0.006 | 0.92 ± 0.07 | 46 ± 6.1 |
| 2AG | 0.06 ± 0.04 | 0.18 ± 0.02 | 65 ± 1.3 |
| AEA | 0.19 ± 0.12 | 0.31 ± 0.14 | 66 ± 5.7 |