Table 2

ED50 values (95% confidence limits; milligrams per kilogram, s.c.) of four currently available antipsychotics for the induction of prolactin release, the antagonism of apomorphine-induced abnormal behaviour, and the occupancy of D2 receptors in the pituitary and the striatum

CompoundED50 for Elevating Prolactin > 20 ng/mlED50 for D2 Receptor
Prolactin ReleaseApomorphine AntagonismRatioPituitaryStriatumRatio
mg/kg, s.c.; 95% CL2-a mg/kg, s.c.; 95% CL2-b
Amisulpride0.001737217640.02617654
(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]
Risperidone0.00500.070140.0810.8911
(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]
Quetiapine0.555.8104.1246
(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]
Olanzapine0.100.171.70.430.300.7
(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.