Table 1.
Binding affinities of SW IV‐134 and SW43 to the sigma‐1 and sigma‐2 receptors.
| Compound | Ki (nM)a | σ1/σ2 d | |
|---|---|---|---|
| σ1 b | σ2 c | ||
| SW 43 | 134.3 ± 11.9 | 7.1 ± 1.3 | 19 |
| SW IV‐134 | 5737 ± 476 | 22.6 ± 1.8 | 253 |
Abbreviations: σ1 for Sigma‐1 receptor. σ2 for Sigma‐2 receptor.
a
Mean ± SEM. Ki values were determined by at least three experiments.
b
Ki for inhibiting the binding of [3H](+)‐pentazocine to guinea pig brain homogenates.
c
Ki for inhibiting the binding of [3H](+)DTG to rat liver homogenates.
d
Ki for σ1 receptors/ Ki for σ2 receptors.