Drug | Internalization | MAPK Activation | β-Arrestin Recruitment | VGCC Inhibition | CB2Ki |
---|---|---|---|---|---|
% basal | membrane/cytosol ratio | % inhibition | nM | ||
CP55,940 | 61 ± 1.9 | 130 ± 3.6*** | 1.9 ± 0.11††† | 17 ± 2.4** | 0.64–2.8a |
WIN55,212–2 | 100 ± 3.2 | 130 ± 4.9** | 1.1 ± 0.035 | −3.4 ± 3.2 | 0.28–16.2a |
AM1241 | 100 ± 6.6 | 100 ± 3.5 | 1.0 ± 0.056 | −0.83 ± 1.1 | 3.4b |
JWH015 | 91 ± 5.8 | 120 ± 2.4*** | 1.1 ± 0.030 | −3.9 ± 2.1* | 14–430a |
JWH133 | 77 ± 3.3 | 120 ± 2.7*** | 1.2 ± 0.058††† | 18 ± 6.2* | 3.4a |
THC | 100 ± 2.0 | 120 ± 2.2*** | 1.1 ± 0.058 | −7.0 ± 2.7 | 1.7–75a |
THCV | 88 ± 2.0 | 120 ± 2.1** | 1.0 ± 0.032 | −17 ± 7.4 | 63–75c |
AM1710 | 71 ± 3.0 | 120 ± 3.2** | 1.3 ± 0.060††† | −3.1 ± 4.1 | 6.7d |
A-836339 | 82 ± 2.1 | 120 ± 2.5*** | 1.2 ± 0.039†† | 16 ± 4.1 | 0.64e |
2-AG | 81 ± 6.3 | 130 ± 8.1* | 1.1 ± 0.025 | 33 ± 6.2* | 140–1400a |
GW405833 | N.D. | N.D. | N.D. | −2.5 ± 1.4 | 12f |
AM630 | 100 ± 2.1 | 97 ± 1.3 | 1.0 ± 0.022 | −12 ± 2.4** | 31a |
SR144528 | 130 ± 4.5 | 99 ± 2.0 | 0.93 ± 0.039 | −10 ± 3.2* | 0.040–15a |
N.D., no data (GW405833 not tested in control cells).
↵* p < 0.05 versus untransfected control cells.
↵** p < 0.01 versus untransfected control cells.
↵*** p < 0.001 versus untransfected control cells.
↵†† p < 0.01 versus untreated control.
↵††† p < 0.001, versus untreated control.
↵a Miller and Stella, 2008.
↵b Ibrahim et al., 2003.
↵c Thomas et al., 2005.
↵d Khanolkar et al., 2007.
↵e Yao et al., 2009.
↵f Gallant et al., 1996.