Table 1. Summary of binding interactions (Ki values) and functional activation ([35S]GTPγS binding assay) of THC and PET diastereoisomers on human CB1R and CB2R.
Emax values represent the maximal [35S]GTPγS binding expressed as percentage of the vehicle-treated sample (100%). “Full” and “partial” in brackets stand for full and partial agonist.
|
Receptor binding Ki values (nM, mean ± SD) |
Receptor activation EC50 (nM) and Emax (%) values (mean ± SD) |
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| Cannabinoid | CB1R | CB2R | CB1R (EC50) | CB1R (Emax) | CB2R (EC50) | CB2R (Emax) |
| CP55,940 | 1.2 ± 0.5 | 0.7 ± 0.3 | 17 ± 9 | 173 ± 6 (full) |
1.9 ± 0.8 | 194 ± 5 (full) |
| Δ9-trans-THC | 22 ± 13 | 47 ± 11 | 43 ± 30 | 146 ± 3 (partial) |
12 ± 7 | 134 ± 4 (partial) |
| Δ9-cis-THC | 228 ± 45 | 99 ± 29 | 552 ± 123 | 158 ± 6 (partial) |
119 ± 69 | 153 ± 5 (partial) |
| trans-PET | 127 ± 82 | 126 ± 55 | 171 ± 116 | 142 ± 5 (partial) |
478 ± 288 | 116 ± 6 (partial) |
| cis-PET | 481 ± 125 | 225 ± 61 | 406 ± 175 | 142 ± 5 (partial) |
167 ± 136 | 113 ± 4 (partial) |