Compound | [125I]RTI-55 Binding HEK-hDAT:Ki (nM) and Hill Slope | [3H]DA Uptake HEK-hDAT: IC50 (nM) and Hill Slope | [125I]RTI-55 Binding HEK hSERT: Ki (nM) and Hill Slope | [3H]5HT Uptake HEK-hSERT: IC50 (nM) and Hill Slope | [125I]RTI-55 Binding HEK-hNET: Ki(nM) and Hill Slope | [3H]Nisoxetine Binding HEK-hNET:Ki (nM) and Hill Slope | [3H]NE Uptake HEK-hNET: IC50 (nM) and Hill Slope |
---|---|---|---|---|---|---|---|
Benztropine | 293 ± 70 | 42 ± 8 | 15,800 ± 3300 | 47,000 ± 14,000 | 4000 ± 1300 | 11,800 ± 1900 | 292 ± 54 |
1.16 ± 0.13 | 0.62 ± 0.07 | 1.25 ± 0.17 | 1.42 ± 0.19 | 0.78 ± 0.05 | 1.30 ± 0.12 | 0.85 ± 0.17 | |
Bupropion | 2630 ± 420 | 2900 ± 840 | 34,600 ± 3300 | 47,000 ± 15,000 | 20,700 ± 7500 | 185,000 ± 17,000 | 1450 ± 380 |
1.09 ± 0.09 | 1.08 ± 0.18 | 1.27 ± 0.15 | 1.13 ± 0.34 | 1.02 ± 0.13 | 1.37 ± 0.12 | 0.89 ± 0.25 | |
CFT | 88.0 ± 7.2 | 27.2 ± 1.7 | 140 ± 35 | 133 ± 31 | 428 ± 69 | 4700 ± 1100 | 33.3 ± 2.3 |
1.20 ± 0.14 | 0.78 ± 0.19 | 1.07 ± 0.04 | 1.12 ± 0.06 | 1.02 ± .15 | 1.14 ± 0.09 | 0.75 ± 0.11 | |
Cocaine | 370 ± 33 | 278 ± 56 | 403 ± 97 | 410 ± 120 | 1600 ± 230 | 20,000 ± 2500 | 910 ± 200 |
0.98 ± 0.03 | 0.98 ± 0.14 | 1.02 ± 0.12 | 0.99 ± 0.15 | 1.21 ± 0.09 | 1.02 ± 0.06 | 0.77 ± 0.10 | |
Desmethyl-imipramine | 14,600 ± 1300 | 82,000 ± 10,000 | 55.4 ± 4.0 | 64 ± 17 | 13.9 ± 1.5 | 4.1 ± 1.2 | 4.2 ± 1.1 |
1.01 ± 0.05 | 2.84 ± 0.45 | 0.86 ± 0.12 | 1.23 ± 0.27 | 1.66 ± 0.44 | 1.08 ± 0.05 | 1.25 ± 0.22 | |
Dopamine (K m) | 6400 ± 590 | 460 ± 110 | 1,110,000 ± 180,000 | 30,800 ± 6100 | 28,000 ± 11,000 | 47,300 ± 3200 | 6.63 ± 0.26 |
1.10 ± 0.02 | 0.76 ± 0.18 | 1.18 ± 0.23 | 1.02 ± 0.39 | 0.70 ± 0.08 | 1.50 ± 0.04 | 0.46 ± 0.04 | |
Fluoxetine | 6670 ± 850 | 19,500 ± 7600 | 1.14 ± 0.53 | 7.3 ± 2.9 | 1560 ± 300 | 1020 ± 180 | |
1.04 ± 0.06 | 0.96 ± 0.17 | 0.75 ± 0.05 | 1.07 ± 0.34 | 1.48 ± 0.16 | 1.08 ± 0.09 | ||
GBR-12935 | 14.2 ± 2.7 | 22.4 ± 5.6 | 385 ± 44 | 6800 ± 3400 | 540 ± 160 | 1330 ± 280 | 235 ± 53 |
1.57 ± 0.75 | 0.81 ± 0.19 | 0.87 ± 0.03 | 1.03 ± 0.45 | 1.31 ± 0.35 | 1.28 ± 0.16 | 0.86 ± 0.21 | |
Imipramine | 25,500 ± 2000 | 25,600 ± 7400 | 3.32 ± 0.44 | 8.0 ± 2.3 | 215 ± 72 | 98 ± 22 | 70 ± 21 |
1.36 ± 0.19 | 1.07 ± 0.11 | 0.82 ± 0.04 | 1.25 ± 0.42 | 1.26 ± 0.24 | 0.92 ± 0.13 | 1.04 ± 0.23 | |
Mazindol | 35 ± 10 | 28.8 ± 7.8 | 95 ± 32 | 160 ± 46 | 12.6 ± 2.0 | 3.42 ± 0.67 | 3.3 ± 1.1 |
0.93 ± 0.02 | 1.16 ± 0.17 | 1.01 ± 0.06 | 0.81 ± 0.15 | 1.27 ± 0.17 | 1.06 ± 0.21 | 1.94 ± 0.34 | |
(+)-Methamphetamine | 5200 ± 1300 | 82.3 ± 8.6 | 122,800 ± 2800 | 20,700 ± 5400 | 1500 ± 260 | 40,300 ± 8000 | 1.27 ± 0.30 |
0.95 ± 0.08 | 0.83 ± 0.05 | 1.21 ± 0.05 | 1.19 ± 0.22 | 0.64 ± 0.07 | 1.79 ± 0.22 | 0.32 ± 0.02 | |
Threo-(±)-methylphenidate | 184 ± 38 | 193 ± 45 | 40,400 ± 8300 | 55,000 ± 16,000 | 1770 ± 780 | 2350 ± 390 | 37.7 ± 4.1 |
0.97 ± 0.04 | 0.97 ± 0.30 | 0.98 ± 0.01 | 0.92 ± 0.22 | 0.70 ± 0.06 | 0.90 ± 0.12 | 0.63 ± 0.08 | |
Nisoxetine | 1690 ± 200 | 497 ± 82 | 73.0 ± 3.3 | 400 ± 150 | 32.5 ± 4.6 | 6.0 ± 0.5 | 5.3 ± 1.6 |
1.08 ± 0.04 | 0.89 ± 0.08 | 0.90 ± 0.08 | 0.78 ± 0.26 | 0.94 ± 0.06 | 0.85 ± 0.05 | 1.51 ± 0.80 | |
Nomifensine | 87 ± 23 | 72 ± 9 | 2350 ± 200 | 2780 ± 650 | 119 ± 16 | 71 ± 6 | 42 ± 15 |
0.99 ± 0.08 | 1.34 ± 0.36 | 1.05 ± 0.11 | 0.88 ± 0.02 | 0.92 ± 0.09 | 0.95 ± 0.11 | 0.93 ± 0.20 | |
Norepinephrine | 57,000 ± 13,000 | 13,700 ± 7600 | 1,470,000 ± 110,000 | 540,000 ± 160,000 | 160,000 ± 33,000 | 399,000 ± 32,000 | 110 ± 21 |
1.02 ± 0.10 | 0.97 ± 0.15 | 2.80 ± 0.56 | 1.10 ± 0.25 | 0.99 ± 0.17 | 1.51 ± 0.24 | 0.85 ± 0.17 | |
Nortriptyline | 4030 ± 960 | 14,500 ± 4400 | 33.0 ± 2.6 | 168 ± 45 | 7.5 ± 2.4 | 17.0 ± 0.5 | 3.50 ± 0.90 |
1.05 ± 0.09 | 2.00 ± 0.73 | 0.72 ± 0.11 | 1.33 ± 0.27 | 0.83 ± 0.08 | 1.02 ± 0.05 | 0.67 ± 0.01 | |
Serotonin | 549,000 ± 96,000 | 15,200 ± 3700 | 3500 ± 1200 | 170 ± 62 | 360,000 ± 71,000 | 840,000 ± 78,000 | 5420 ± 840 |
1.17 ± 0.08 | 0.85 ± 0.07 | 0.99 ± 0.12 | 0.88 ± 0.19 | 0.85 ± 0.15 | 1.79 ± 0.27 | 0.60 ± 0.13 | |
RTI-55 | 2.3 ± 0.7 | 3.3 ± 1.0 | 0.55 ± 0.03 | 0.51 ± 0.14 | 19.0 ± 3.7 | 140 ± 3 | 2.63 ± 0.76 |
1.11 ± 0.08 | 1.34 ± 0.29 | 0.93 ± 0.16 | 1.05 ± 0.13 | 0.85 ± 0.09 | 0.82 ± 0.03 | 1.13 ± 0.22 |
Values are the mean ± S.E.M. of three to eight experiments.