TABLE 1

SoRI analogs partially inhibit DAT binding

[125I]RTI-55 binding to membranes prepared from hDAT HEK cells was conducted as described under Materials and Methods. Ten-point inhibition curves were generated for each test drug using three concentrations of [125I]RTI-55. The data were transformed to percentage of inhibition and fit to the dose-response curve for the best-fit estimates of the EC50 and Emax values, using KaleidaGraph version 3.60.4. All curves were based on an n = 4, except for cocaine (n = 3). Each value is ±S.D.


Compound

EC50

Emax
nM %
Cocaine
    0.01 nM [125I]RTI-55 290 ± 18 101 ± 2
    0.11 nM [125I]RTI-55 439 ± 43* 102 ± 3
    1.0 nM [125I]RTI-55 985 ± 175* 98 ± 6
SoRI-2827
    0.01 nM [125I]RTI-55 1922 ± 390 77 ± 4
    0.11 nM [125I]RTI-55 1765 ± 267 75 ± 3
    1.0 nM [125I]RTI-55 3080 ± 1245 39 ± 4*
SoRI-20040
    0.01 nM [125I]RTI-55 1559 ± 247 87 ± 3
    0.11 nM [125I]RTI-55 1786 ± 319 81 ± 4
    1.0 nM [125I]RTI-55 2969 ± 344* 62 ± 2*
SoRI-20041
    0.01 nM [125I]RTI-55 1377 ± 144 69 ± 2
    0.11 nM [125I]RTI-55 1983 ± 270* 66 ± 2
    1.0 nM [125I]RTI-55
3077 ± 795*
44 ± 3*
  • * p < 0.05 (Student's t test) compared with the 0.01 nM [125I]RTI-55 condition.

  • p < 0.05 (Student's t test) compared with the 0.11 nM [125I]RTI-55 condition.