TABLE 5

SoRI compounds noncompetitively inhibit [3H]DA uptake

Uptake binding surfaces were generated as described under Materials and Methods in the absence and presence of the indicated concentrations of test drugs. The data of three experiments (132 data points) were pooled and fit to the one-component uptake equation for the best-fit estimates of the Vmax and Km values. Each value is ±S.D., n = 3.


Condition

Vmax

Apparent KM
% of control nM
SoRI-20040
    Control 100 ± 7 36.8 ± 1.4
    0.8 μM 74 ± 7* 50.7 ± 2.2*
    3.2 μM 39 ± 2* 48.6 ± 3.0*
    12.8 μM 22 ± 2* 50.4 ± 5.0*
SORI-20041
    Control 100 ± 5 52.9 ± 3.0
    0.8 μM 30 ± 2* 65.7 ± 5.1*
    3.2 μM 22 ± 4* 78.5 ± 8.9*
    12.8 μM 16 ± 2* 87.4 ± 9.0*
SORI-2827
    Control 100 ± 7* 41.7 ± 2.1
    0.8 μM 98 ± 7 72.1 ± 2.3*
    3.2 μM 92 ± 6 89.8 ± 3.5*
    12.8 μM
68 ± 4*
84.6 ± 5.6*
  • * p < 0.01 (F-test).