Table 2.
In vitro pharmacology data for cannabinoid 2 receptor (CB2R) agonists HU308, HU910, RO6871304, RO6871085, and CB2R inverse agonist RO6851228. (These data have been generated at the Roche Laboratories and were partially published, see also [28,29,32]). Due to their relevance for the described pharmacology studies, they are provided here in a condensed format. * Indicates previously published data.
| Compound | HU308 | HU910 | RO6871304 | RO6871085 | RO6851228 |
|---|---|---|---|---|---|
| hCB2R: Ki (nM) | 10 * | 43 * | 17 | 76 * | 45 * |
| hCB1R: Ki (nM) | 4600 * | 3734 * | >10,000 * | 3378 * | 6487 * |
| hCB1R Ki/hCB2R Ki | 460 | 89 | >588 * | 44 * | 147 * |
| mouse CB2R: Ki (nM) | 223 | 276 | 34 | 6 * | 1 * |
| hCB2R: cAMP EC50 (nM), efficacy (%) | 3, 98 * | 4, 98 * | 1, 102 * | 8, 88 * | 26, −159 * |
| hCB1R: cAMP EC50 (nM) | >10,000 * | >10,000 * | >10,000 * | 1449, 38 * | >10,000 |
| hCB1R cAMP EC50/hCB2R cAMP EC50 | >3333 | >2500 | >10,000 | 174 * | >383 * |
| mouse CB2R: cAMP EC50 (nM), efficacy (%) | 6, 99 | 3, 99 | 0.5, 101 | 3, 81 * | 4, −174 * |
| hCB2R: beta arrestin EC50 (nM), efficacy (%) | 101, 107 * | 109, 81 * | 21, 119 * | 55, 51 | 3, −18 |
| hCB1R: beta arrestin EC50 (nM) | >10,000 * | >30,000 * | >30,000 | >30,000 * | n.d. |
| hCB1R beta arrestin EC50/hCB2R beta arrestin EC50 | >99 | >275 | >1429 | >545 | n.d. |
| mouse CB2R: beta arrestin EC50 (nM), efficacy (%) | 592, 76 | 224, 54 | 26, 94 | >30,000 | >30,000 |