Table 5.
Interaction of Mefloquine and other drugs with recombinant human dopamine receptors
| Drug | D1 [3H]SCH23390 |
D2 [3H]YM 09151-2 |
D3 [3H]YM 09151-2 |
D4.4 [3H]YM 09151-2 |
|---|---|---|---|---|
| Ki (nM) ± SEM | ||||
| (+)-Mefloquine | >10 μM | >10 μM | 1960 ± 230 | >10 μM |
| (−)-Mefloquine | >10 μM | >10 μM | >10 μM | >10 μM |
| Chloroquine | >10 μM | >10 μM | >10 μM | >10 μM |
| LSD | 273 ± 89 | 38.8 ± 1.8 | 27.1 ± 1.3 | 330 ± 120 |
| DA | 4300 ± 1000 | 1710 ± 150 | 61 ± 20 | 630 ± 180 |
| SKF 38393 | 258 ± 51 | 4800 ± 2600 | 4300 ± 1800 | 28000 ± 13000 |
| SCH23390 | 0.491 ± 0.087 | 887 ± 17 | 1920 ± 580 | 9700 ± 1100 |
| Quinpirole | >10 μM | 2780 ± 510 | 52.8 ± 6.1 | 262 ± 66 |
| Butaclamol | 4.1 ± 2.0 | 2.04 ± 0.40 | 4.0 ± 1.3 | 255 ± 63 |
Radioligand binding assays were conducted as described in the text. Each Ki value represents the mean of at least 3 independent experiments, each conducted with duplicate determinations. For purposes of comparison, agonists and antagonists for each receptor were included in the assays (D1 receptor: SKF 38393 and SCH 23390; D2, D3 and D4.4 receptor: quinpirole and butaclamol). Abbreviations: SCH23390 7-chloro-3-methyl-1-phenyl-1,2,4,5-tetrahydro-3-benzazepin-8-ol; YM-09151-2 nemonapride N-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-(methylamino)benzamide; LSD lysergic acid diethylamide; DA dopamine; SKF38393 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol.