TABLE 2.
Inhibition by various dopamine uptake inhibitors of specific binding of [3H]WIN35428 and [3H]JHW 007 in rodent striatal membranes
Values in parentheses are 95% confidence limits.
|
Ki Value
|
|||||
|---|---|---|---|---|---|
| [3H]WIN 35428
|
[3H]JHW 007
|
||||
| Rat | Mouse | Rat | Mouse | ||
| nM | |||||
| Dopamine uptake inhibitors | |||||
| Cocaine | Ki 1 | 87.5 (82.0–93.3) | 80.4 (69.8–92.7) | 20.2 (15.5–26.5) | 27.5 (18.7–40.6) |
| Ki 2 | 33,000 (20,100–54,000) | 19,200 (11,100–33,300) | |||
| GBR 12909 | Ki 1 | 3.24 (2.84–3.70) | 3.47 (3.03–4.04) | 11.6 (1.14–117) | 0.247 (0.0186–3.26) |
| Ki 2 | 15.5 (1.49–162) | 7.01 (5.21–9.44) | |||
| Mazindol | Ki 1 | 3.10 (2.90–3.31) | 10.4 (9.12–11.7) | 3.64 (2.48–5.33) | 19.5 (15.2–25.1) |
| Ki 2 | 557 (378–822) | 9350 (5830–15,000) | |||
| Nomifensine | Ki 1 | 30.1 (27.2–33.3) | 27.5 (25.7–29.3) | 43.5 (30.3–62.4) | 30.6 (23.9–38.9) |
| Ki 2 | 4610 (2520–8430) | 9640 (4730–19,600) | |||
| Norcocaine | Ki 1 | 153 (139–168) | 154 (144–165) | 142 (97.5–127) | 116 (93.3–144) |
| Ki 2 | 9330 (5190–16,800) | 20,900 (11,200–38,900) | |||
| WIN 35065-2 | Ki 1 | 29.4 (27.1–31.9) | 26.3 (23.4–29.6) | 26.1 (19.7–34.5) | 47.3 (28.2–79.1) |
| Ki 2 | 40,600 (17,900–92,000) | 30,000 (17,600–50,900) | |||
| WIN 35428 | Ki 1 | 11.8 (8.95–15.5) | 21.9 (12.7–37.7) | ||
| Ki 2 | 23,900 (13,100–43,600) | 20,700 (13,600–31,400) | |||
| RTI-55 | Ki 1 | 1.12 (0.993–1.26) | 0.714 (0.637–0.800) | 1.08 (0.753–1.55) | 0.831 (0.653–1.06) |
| Ki 2 | 6370 (4700–8240) | 8150 (6240–10,600) | |||
| Serotonin uptake inhibitors | |||||
| Paroxetine | Ki 1 | 560 (515–610) | 408 (374–446) | 316 (225–442) | 640 (516–793) |
| Ki 2 | 7740 (4060–14,700) | 39,100 (16,000–95,100) | |||
| Citalopram | Ki 1 | 11,400 (9820–13,200) | 8970 (7850–10,300) | 12,800a (11,100–14,900) | 4660 (851–25,500) |
| Ki 2 | 15,600 (3810–64,300) | ||||
| Fluoxetine | Ki | 2470 (2140–2860) | 1120 (979–1290) | 3480b (2990–4050) | 3600a (2420–5350) |
| Norepinephrine uptake inhibitors | |||||
| Desmethylimipramine | Ki 1 | 1960 (1670–2290) | 1310 (1120–1530) | 162 (22.8–1160) | 1010 (469–2180) |
| Ki 2 | 3860 (2470–6050) | 13,200 (4680–37,400) | |||
| Nisoxetine | Ki 1 | 163 (151–175) | 149 (135–165) | 226 (187–273) | 239 (193–297) |
| Ki 2 | 16,400 (7930–33,800) | 16,000 (10,400–25,800) | |||
| Atomoxetine | Ki 1 | 492 (456–531) | 593 (543–647) | 685 (556–845) | 573 (460–714) |
| Ki 2 | 33,800 (11,400–99,800) | 43,300 (19,100–97,900) | |||
| Benztropine analogs | |||||
| 4′-Cl-BZT | Ki 1 | 19.0 (17.5–21.6) | 17.7 (15.8–19.8) | 26.0 (23.0–29.3) | 24.6 (20.8–29.0) |
| Ki 2 | 5330 (2140–13,300) | 1190 (514–2770) | |||
| AHN 1-063 | Ki 1 | 399 (369–433) | 341 (316–368) | 270 (198–369) | 253 (206–310) |
| Ki 2 | 5060 (670–38,200) | 13,300 (2700–65,300) | |||
| JHW 007 | Ki | 12.0 (11.2–12.8) | 11.7 (10.5–13.0) | ||
a
These data did not converge on a two-site model. Values for a single-site model are listed.
b
The variance accounted for by a two-site model was greater than that accounted for by a one-site model. However, the values provided by the two-site model varied from each other by less than 5%, and the variability around the fitted constants was extremely large. Therefore, values for the constants provided by the single-site model are listed.