Table 1

Effect of SCH-202676 on antagonist binding to GPCRs

ReceptorG-Protein CouplingRadiolabeled LigandIC50n
μM
δ-OpioidGi [3H]Diprenorphine0.3  ± 0.043
κ-OpioidGi [3H]Diprenorphine1.7  ± 0.094
μ-OpioidGi [3H]Diprenorphine1.8  ± 0.024
M1 Gq [3H]N-Methylscopolamine0.42
M2 Gi [3H]N-Methylscopolamine0.42
α2a-AdrenergicGi [3H]Yohimbine0.5  ± 0.14
β1-AdrenergicGs [125I]Idocyanopindolol1.2  ± 0.034
D1 Gs [3H]SCH-233900.1  ± 0.04
D2 Gi [3H]Methylspiperone0.1  ± 0.04

Binding assays were performed as described under Experimental Procedures using recombinant human receptors. Data shown are mean ± S.E. n = number of observations.