Table 1.
Competition binding between ospemifene, raloxifene, nafoxidine, and bazedoxifene and the CBR agonist [3H]CP-55,940 employing CHO-hCB1 and CHO-hCB2 membranes.
| Drug | [3H]CP-55,940 Binding |
||||||
|---|---|---|---|---|---|---|---|
| CHO-hCB1 |
CHO-hCB2 |
Selectivity | |||||
| Ki (nM) | pKi | N | Ki (nM) | pKi | N | (CB1/CB2) | |
| OSP | 753 | 6.123 ± 0.060a | 5 | 3715 | 5.430 ± 0.033a,∗∗ | 3 | 0.20 |
| RAL | 210 | 6.677 ± 0.063b | 4 | 240 | 6.620 ± 0.037b | 3 | 0.88 |
| NAF | 957 | 6.019 ± 0.084a | 3 | 1300 | 5.886 ± 0.044c | 3 | 0.74 |
| BAZ | 836 | 6.078 ± 0.066a | 5 | 254 | 6.595 ± 0.023b,∗∗ | 5 | 3.29 |
a,b,cpKi values designated by different letters are significantly different from values in the same column; P < 0.05, one-way ANOVA, Tukey Post-hoc test. ∗∗ pKi values for individual SERMs examined at hCB2 receptors are significantly different from pKi values for same compounds at hCB1 receptors; P < 0.01, student’s t-test.