Inhibition of specific [125I]PE2I binding in rat striatal membranes
| Drug | Ki |
|---|---|
| nM | |
| PE2I | 6.8 ± 0.4 |
| GBR 12909 | 1.3 ± 0.3 |
| β-CIT | 1.4 ± 0.8 |
| Cocaine | 480 ± 28 |
| Paroxetine | 416 ± 76 |
| Nisoxetine | 450 ± 50 |
| Haloperidol | >1000 |
| Sulpiride | >1000 |
| SCH 23390 | >1000 |
A mixture of 20 pM [125I]PE2I and 4 nM unlabeled PE2I was incubated with 30 μg of protein in Tris · HCl buffer, pH 7.4, for 90 min at 22°C in the presence of different drugs at concentrations of 10−5 to 10−10 M. Total binding was determined in the absence of drugs, and nonspecific binding was determined in the presence of 30 μM cocaine. IC50 values were determined graphically, and the Ki values were calculated according to the method of Cheng and Prussoff (1973):Ki = 1/[1 + (1/Kd)].
Values are mean ± S.D. of 3 independent experiments, each performed in triplicate.