Comparison of Ki values at DAT, NET, and SERT
Propensity of sydnocarb, various DAT inhibitors, and d-AMPH to produce RHS (present study; Gruner et al., 2009) and their estimated Ki values at DAT, NET, and SERT in mice or rats (Pan et al., 1994; Nishino et al., 1998; Rothman and Baumann, 2003; Han and Gu, 2006). Values in parentheses represent ratios of Ki values at NET or SERT over Ki values at DAT.
| Compound | RHS | Uptake Inhibition Ki Values | ||
|---|---|---|---|---|
| DAT | NET | SERT | ||
| nM | ||||
| Sydnocarb | No | 8.3 | 1500 (181) | >10,000 (>1205) |
| GBR-12909 | No | 4.3 | 79.2 (18.4) | 73.2 (17.0) |
| GBR-12935 | No | 4.9 | 277 (56.5) | 289 (59.0) |
| Mazindol | No | 25.9 | 2.9 (0.1) | 272 (10.5) |
| Nomifensine | No | 93.1 | 32 (0.3) | 1889 (20.3) |
| Cocaine | Yes | 478 | 779 (1.6) | 304 (0.6) |
| Methylphenidate | Yes | 260 | 170 (0.7) | 1143 (4.4) |
| Bupropion | Yes | 1534 | >10,000 (>6.5) | 34,707 (22.6) |
| d-AMPH | Yes | 550 | 120 (0.2) | 2382 (4.3) |