Compound | ED50 for Elevating Prolactin > 20 ng/ml | ED50 for D2 Receptor | ||||
---|---|---|---|---|---|---|
Prolactin Release | Apomorphine Antagonism | Ratio | Pituitary | Striatum | Ratio | |
mg/kg, s.c.; 95% CL2-a | mg/kg, s.c.; 95% CL2-b | |||||
Amisulpride | 0.0017 | 37 | 21764 | 0.026 | 17 | 654 |
(0.00074–0.0037) | (28–51) | (0.017–0.038) | (15–19) | |||
[r 2: 0.90; p: 0.12] | [r 2: 0.98; p: 0.76] | |||||
Risperidone | 0.0050 | 0.070 | 14 | 0.081 | 0.89 | 11 |
(0.0032–0.0077) | (0.047–0.102) | (0.053–0.122) | (0.68–1.17) | |||
[r 2: 0.90; p: 0.14] | [r 2: 0.96; p: 0.94] | |||||
Quetiapine | 0.55 | 5.8 | 10 | 4.1 | 24 | 6 |
(0.30–1.00) | (4.6–7.1) | (2.4–7.1) | (14–40) | |||
[r 2: 0.84; p: 0.063] | [r 2: 0.88; p: 0.063] | |||||
Olanzapine | 0.10 | 0.17 | 1.7 | 0.43 | 0.30 | 0.7 |
(0.058–0.19) | (0.12–0.23) | (0.37–0.49) | (0.26–0.36) | |||
[r 2: 0.98; p: 0.75] | [r 2: 0.98; p: 0.27] |
CL, confidence limits.
↵2-a ED50 values were determined from the fraction of rats achieving a biologically significant (>20 ng/ml) prolactin elevation using two to three doses over a 4- to 16-fold range.
↵2-b ED50 values were determined from the sigmoidal log dose-receptor occupancy curve (Fig. 1) of best fit by nonlinear regression analysis with the GraphPad Prism program. Note a p value >0.05 means that the data does not systematically deviate from the sigmoidal curve.