TABLE 1.
Membrane binding constants for [3H]WIN35428 and [3H]JHW 007
Cells without entries indicate that single-component kinetic or single-site binding models were preferred.
| [3H]WIN 35428
|
[3H]JHW 007
|
||||||
|---|---|---|---|---|---|---|---|
| Rat | Swiss-Webster Mouse | Rat | Swiss-Webster Mouse | hDAT/N2A | DAT WT | DAT KO | |
| Association kon 1 (nM−1 · min−1) | 0.246 (±0.0220) | 0.236 (±0.0233) | 5.35 (±4.22) | 7.10 (±10.7) | 2.13 (±1.03) | N.D. | N.D. |
| Half-life (min) | 2.82 | 2.94 | 0.130 | 0.0977 | 0.326 | N.D. | N.D. |
| Y-Max (dpm) | 2560 (±42.1) | 1450 (±26.1) | 1700 (±143) | 1370 (±135) | 5180 (±888) | N.D. | N.D. |
| Association kon 2 (nM−1 · min−1) | 0.0166 (±4.49 × 10−3) | 0.0247 (±6.75 × 10−3) | 0.0563 (±0.0252) | N.D. | N.D. | ||
| Half-life (min) | 41.7 | 28.0 | 12.3 | N.D. | N.D. | ||
| Y-Max (dpm) | 2140 (±218) | 1590 (±157) | 4890 (±851) | N.D. | N.D. | ||
| Dissociation koff 1 (min−1) | 0.181 (±0.0127) | 2.51 (±1.93) | 0.0569 (±7.81 × 10−3) | 0.433 (±0.251) | 1.43 (±0.883) | N.D. | N.D. |
| Half-life (min) | 3.83 | 0.277 | 12.2 | 1.60 | 0.484 | N.D. | N.D. |
| Dissociation koff 2 (min−1) | 0.162 (±0.0185) | 0.0319 (±0.0214) | 0.0726 (±0.0135) | N.D. | N.D. | ||
| Half-life (min) | 4.28 | 21.7 | 9.54 | N.D. | N.D. | ||
| Kd 1 (nM) | 4.21 (±0.0334) | 8.99 (±0.0410) | 7.40 (±0.0533) | 8.18 (±0.057) | 43.7 (±0.0677) | 25.1 (±0.0524) | 28.4 (±0.0751) |
| Bmax 1 (fmol/mg protein) | 1860 (±27.5) | 1860 (±29.1) | 9230 (±115) | 13,200 (±241) | 52,200 (±1260) | 22,300 (±408) | 11,100 (±356) |
| Hill slope | 0.958 (±0.0268) | 0.918 (±0.0256) | 0.734 (±0.0393) | 0.550 (±0.0348) | 1.44 (±0.146) | 0.813 (±0.0482) | 0.552 (±0.0418) |
| Kd 2 (nM) | 4400 (±0.338) | 2750 (±0.195) | 2380 (±0.317) | 2000 (±0.149) | |||
| Bmax 2 (fmol/mg protein) | 787,000 (±59,200) | 1.09 × 106 (±68,900) | 459,000 (±48,500) | 493,000 (±30,600) | |||
N.D., not determined.