TABLE 2.
Inhibition of the binding of radioligands labeling σ1 and σ2 receptors
Values in parentheses are 95% confidence limits.
| Compound | σ1R Ki Value Determined with [3H]Pentazocine | σ2R Ki Value Determined with [3H]DTG |
|---|---|---|
| nM | ||
| PRE-084 | 48.5 (39.8–59.2) | 12,700 (9290–17,300) |
| (+)-Pentazocine | 4.59 (4.26–4.97) | 224 (195–257) |
| d-Methamphetamine | 4390 (3740–5160) | 15,900 (11,700–21,500) |
| Heroin | N.D. | 68,600 (27,100–173,000) |
| Ketamine | 227,000 (53,400–963,000) | 36,900 (20,100–67,900) |
| (+)-Butaclamol | 4700 (4270–5170) | 2100 (1770–2498) |
| Naltrexone | N.D. | <50% displacement at 10 mM |
N.D., no displacement at concentrations up to 10 mM.