TABLE 2.
Compound(s) | hCB1R | hCB2R | ||
---|---|---|---|---|
IC50 (nM) (95% C.I.) | E min (% CP55,940) ± S.E.M | IC50 (nM) (95% C.I.) | E min (% CP55,940) ± S.E.M | |
CP55,940 | 6.6 (2.7–15) | 0.0 ± 5.6 | 40 (7.7–220) | 1.5 ± 14.3 |
EC21a | n.c | 103 ± 2.5*** | 36 (4.6–77) | 115 ± 7.9*** |
LV62 | n.c | 106 ± 3.6*** | 0.65 (0.13–34) | 16 ± 11.9 |
JR14a | n.c | 98 ± 2.5*** | 1.8 (0.26–6.2) | 59 ± 12.3* |
JR64a | n.c | 104 ± 4.7*** | 0.60 (0.20–26) | 20 ± 10.3 |
Competition binding of [3H]CP55,940 to hCB1R and hCB2R was quantified in membranes derived from CHO-K1 hCB1R or hCB2R cells incubated with compounds for 2 h. Data were fit to a three-parameter non-linear regression in GraphPad (v. 9.0). Data are mean with 95% C.I. (IC50) or mean ± S.E.M, n ≥ 3 independent experiments performed in duplicate. Statistical analyses were by non-overlapping C.I. or two-way ANOVA followed by Bonferroni’s post-hoc test. *p < 0.05, ***p < 0.001 relative to CP55,940 within receptor. Data from this Table are graphed in Figure 4 n. c, not converged. E min values for data that were not fit to a non-linear regression are the mean from the minimum value observed.