TABLE 2

Biased agonism by cannabinoids (KA estimated from the operational model of agonism)

LogR (τ/KA), ΔLogRτ/KA), ΔΔLogR (ΔΔτ/KA) ratios and bias factors (BF) for cannabinoid ligands, relative to 2-AG, at the CB1R were obtained by fitting the data to an operational model of agonism (eq. 5). Values represent the mean ± S.E.M. from at least four independent experiments carried out in triplicate.

LigandcAMPpERK1/2cAMP/pERK1/2
LogRΔLogRLogRΔLogRΔΔLogRBF
CP559408.3 ± 0.22.6 ± 0.27.9 ± 0.12.0 ± 0.10.6 ± 0.23.9
HU-2108.8 ± 0.23.1 ± 0.27.6 ± 0.11.8 ± 0.11.3 ± 0.2*20.8
WIN55,212-26.9 ± 0.21.2 ± 0.26.8 ± 0.11.0 ± 0.10.2 ± 0.21.7
Δ9-THC7.1 ± 0.31.4 ± 0.36.5 ± 0.20.6 ± 0.20.8 ± 0.45.6
Methanandamide6.9 ± 0.21.2 ± 0.25.9 ± 0.20.0 ± 0.21.2 ± 0.3*15.1
Anandamide6.3 ± 0.20.6 ± 0.25.6 ± 0.1−0.3 ± 0.10.8 ± 0.26.8
2-AG5.7 ± 0.20.0 ± 0.25.9 ± 0.10.0 ± 0.10.0 ± 0.21.0
  • * P < 0.05, one-way analysis of variance with Bonferroni’s multiple comparison test between ΔΔLogR for 2-AG compared with other cannabinoids.