Table 5 Signaling parameters for the assays using mouse striatal membranes and mouse primary striatal neurons.

U69,593 serves as the reference agonist. Data are presented as means ± SEM from n ≥ 4 independent experiments. G, [35S]GTPγS binding; cAMP, forskolin-stimulated cAMP accumulation; KORint, KOR internalization; 95% CI, 95% confidence interval.

Compound[35S]GTPγS bindingΔΔLog(Emax/EC50) (G/cAMP, 95% CI)Bias factor (G/cAMP)
EC50 (nM)Emax (%)Log(Emax/EC50)ΔLog(Emax/EC50)
U69221 ± 261008.68 ± 0.06001
1.1486 ± 98*141 ± 538.51 ± 0.07−0.17 ± 0.03−0.02 (−0.25 to 0.10)1.0
CompoundInhibition of cAMP accumulationΔΔLog(Emax/EC50) (G/KORint)Bias factor (G/KORint)
EC50 (nM)Emax (%)Log(Emax/EC50)ΔLog(Emax/EC50)
U6917 ± 41007.76 ± 0.09001
1.145 ± 12167 ± 207.57 ± 0.15−0.19 ± 0.11.3724
CompoundKOR internalizationΔΔLog(Emax/EC50) (cAMP/KORint)Bias factor (cAMP/KORint)
EC50 (nM)Emax (%)Log(Emax/EC50)ΔLog(Emax/EC50)
U69191009.73001
1.1238378.19−1.541.3623

*P < 0.05, Student’s t test for U69,593 versus triazole 1.1.

†Values were obtained from the concentration response curve of which each data point is from the average of n ≥ 3 independent neuron preparations.