Table 3

Stimulation of [35S]GTPγS binding by BU48 acting at recombinant δ-, μ-, or κ-opioid receptors

EC50Maximal Effect3-a
nM %
C6δ0.81  ± 0.2739.7  ± 2.0
C6μ0.085  ± 0.05310.0  ± 3.3
CHOκ0.78  ± 0.2258.6  ± 6.6

Membranes from C6δ, C6μ, or CHO-hkor cells were incubated with [35S]GTPγS (0.1 nM), GDP (30 μM), and varying concentrations of BU48 for 60 min at 30°C as described underMaterials and Methods. Data represent means ± S.E. from three determinations.

  • 3-a  Percentage of response caused by a maximal (10 μM) concentration of SNC80 (C6δ), fentanyl (C6μ), or U69593 (CHOκ).