Inhibition of binding of radioligands labeling DAT, σ1, and σ2 receptors
Values are Ki values, except as indicated, for displacement of the listed radioligands. Values in parentheses are 95% confidence limits, except as indicated. Values listed from previous studies were obtained in this laboratory with conditions identical to the ones presently employed.
| Compound | DAT Ki Value [3H]WIN35,428 | σ1R Ki Value [3H](+)-Pentazocine | σ2R Ki Value (High Affinity)a [3H]DTG |
|---|---|---|---|
| nM | |||
| Cocaineb | 76.6 (72.6–80.5) | 5190 (3800–7060) | 19,300 (16,000–23,300) |
| WIN35,428 | 5.24 (4.92–5.57)b,c | 5700 (4060–8020) | 4160 (3120–5550) |
| d-Methamphetamined | NT | 4390 (3740–5160) | 15,900 (11,800–21,500) |
| JHW007 | 12.0 (11.2–12.8)e | 2.40 (2.07–2.80) | 12.0 (10.0–14.4) |
| AHN2-005 | 8.82 (8.13–9.56) | 15.5 (13.2–18.3) | 28.5 (23.6–34.4) |
| AHN1-055 | 4.09 (3.67–4.56) | 119 (98.9–142) | 78.7 (50.6–122) |
| Heroin | NT | ND | 68,600 (27,100–173,000) |
| Ketamine | NT | 227,000 (53,400–963,000) | 36,900 (20,100–67,900) |
ND, no displacement at concentrations up to 10 mM; NT, not tested.
↵a The value for displacement of DTG is a high-affinity site if the data modeled better for two than one site. The high-affinity site is similar to the site previously identified as the σ2 site.
↵b All values are from Garces-Ramirez et al. (2011).
↵c Value is a Kd value obtained by homologous competition experiments.
↵d Values from Hiranita et al. (2013).
↵e Values from Kopajtic et al. (2010).