Compound | [^{35}S]GTPγS binding | ΔΔLog(E_{max}/EC_{50}) (G/cAMP, 95% CI) | Bias factor (G/cAMP) | |||

EC_{50} (nM) | E_{max} (%) | Log(E_{max}/EC_{50}) | ΔLog(E_{max}/EC_{50}) | |||

U69 | 221 ± 26 | 100 | 8.68 ± 0.06 | 0 | 0 | 1 |

1.1 | 486 ± 98* | 141 ± 53 | 8.51 ± 0.07 | −0.17 ± 0.03 | −0.02 (−0.25 to 0.10) | 1.0 |

Compound | Inhibition of cAMP accumulation | ΔΔLog(E_{max}/EC_{50}) (G/KORint) | Bias factor (G/KORint) | |||

EC_{50} (nM) | E_{max} (%) | Log(E_{max}/EC_{50}) | ΔLog(E_{max}/EC_{50}) | |||

U69 | 17 ± 4 | 100 | 7.76 ± 0.09 | 0 | 0 | 1 |

1.1 | 45 ± 12 | 167 ± 20 | 7.57 ± 0.15 | −0.19 ± 0.1 | 1.37 | 24 |

Compound | KOR internalization | ΔΔLog(E_{max}/EC_{50}) (cAMP/KORint) | Bias factor (cAMP/KORint) | |||

EC_{50} (nM)^{†} | E_{max} (%)^{†} | Log(E_{max}/EC_{50})^{†} | ΔLog(E_{max}/EC_{50})^{†} | |||

U69 | 19 | 100 | 9.73 | 0 | 0 | 1 |

1.1 | 238 | 37 | 8.19 | −1.54 | 1.36 | 23 |

**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.