TABLE 5.
Potencies of various ligands in displacement of [3H]JHW 007 from striatal tissue of WT and DAT KO mice
All values are expressed as nM concentrations. The listed Ki values are those obtained for these compounds as reported in the literature.
| Target | Displacer | IC50 Value (95% confidence interval)
|
Literature Ki Values at Target (± S.E.M.) | |
|---|---|---|---|---|
| DAT KO | WT | |||
| Dopamine D3 | PD 128907 | >10,000 | >10,000 | 8.48 ± 0.11 (Cussac, 2000) |
| Dopamine D2 | L-741626 | 8240 (6200–11,000) | 5130 (3780–6980) | 7.52 ± 0.01 (Cussac, 2000) |
| Histamine H1 | (+)-Chlorpheniramine | >10,000 | >10,000 | 10 (Hill and Young, 1980) |
| Muscarinic M2 | AQ-RA 741 | >10,000 | >10,000 | 8.37 ± 0.04 (Dorje, et al., 1990) |
| 5-HT2A | Ketanserin | >10,000 | >10,000 | 8.86 ± 0.08 (Hoyer, et al., 1985) |
| Sigma | Rimcazole | 4790 (3490–6570) | 1770 (1160–2710) | 836 ± 44 (DeHaven-Hudkins, et al., 1992) |
| Na channel | Tetracaine | >10,000 | >10,000 | 1700 ± 0.6 (Postma and Catterall, 1984) |