Table 1

Binding affinity (pKi and ED50 values) of six antipsychotic drugs for DA and 5-HT receptor subtypes

DrugpKi ValuesED50 Values
D1D2D3D45-HT1A5-HT2A5-HT2C5-HT2A-D2D25-HT2A5-HT2A/D2
APZ6.26.36.31-a 5.91-a 8.05.91.7>1001.1<0.01
CLOZ6.87.06.41-b 8.06.71-b 8.38.11.35.20.90.2
RISP6.21-b 8.97.91-b 7.86.61-b 10.17.51.20.30.10.2
OLAN6.61-b 7.81-b 7.31-b 7.61-b <6.01-c 8.71-b 8.11-b 0.91560.4
HAL7.09.07.71-b 8.05.51-b 7.75.6−1.30.21510
SUL<5.01-d 7.81-d 7.61-d 6.01-d <5.0<5.0<−3.086>340>3.9
  • The pKi values for D1, D2, D4, 5-HT2A, and 5-HT2C receptors were obtained from Meltzer et al. (1989), Stockmeier et al. (1993), Roth et al. (1992, 1995), except where noted. The ED50 values (mg/kg) for in vivo 5-HT2A and D2 receptor occupancy were obtained fromStockmeier et al. (1993) except for OLAN. Data for OLAN refers toBymaster et al. (1996b). The ED50 values of sulpiride are data of a racemic compound.

  • 1-a Data refers to Leysen et al. (1993).

  • 1-b Data refers to Schotte et al. (1996).

  • 1-c Data refers to Bymaster et al. (1996a).

  • 1-d Data refers to Seeman and Van Tol (1995).