Table 1.

SoRI-Analogs Partially Inhibit DAT Binding

Cocaine	EC50 (nM)	EMAX (%)
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*†

[¹²⁵I]RTI-55 binding to membranes prepared from hDAT HEK cells was conducted as described in Methods. Ten point inhibition curves were generated for each test drug using three concentrations of [¹²⁵I]RTI-55. The data were transformed to percent inhibition and fit to the dose-response curve for the best-fit estimates of the EC₅₀ and E_MAX, using Kaleidagraph (Version 3.6.4). All curves were an n=4, except for cocaine (n=3). Each value is ±SD.

^*p<0.05 when compared to the 0.01 nM [¹²⁵I]RTI-55 condition.

^†p<0.05 when compared to the 0.11 nM [¹²⁵I]RTI-55 condition. Students t-test.