TABLE 2

Summary of results obtained for the 36 partial-efficacy DAT uptake blockers

Dose-response curves for each indicated agent were generated as described in Materials and Methods for DAT, NET, and SERT uptake inhibition and DAT binding. Each value is the mean ± S.D.; n = 3.

DrugDAT Uptake IC50DAT Uptake EmaxNET Uptake IC50NET Uptake EmaxSERT Uptake IC50SERT Uptake EmaxDAT Binding IC50DAT Binding Emax5-HT/DA IC50 (Uptake)NE/DA IC50 (Uptake)
nM%nM%nM%μM%
SRI-29070174 ± 5866 ± 41740 ± 115064 ± 10699 ± 16448 ± 31.8 ± 0.471 ± 4410
SRI-29072212 ± 4971 ± 35850 ± 174662 ± 56382 ± 263656 ± 92.7 ± 0.377 ± 23028
SRI-2915320 ± 173 ± 1181 ± 4673 ± 437 ± 1855 ± 51.7 ± 0.276 ± 21.99
SRI-2915510 ± 1.074 ± 1290 ± 5270 ± 368 ± 1354 ± 20.9 ± 0.287 ± 46.829
SRI-29212672 ± 20467 ± 48126 ± 227364 ± 53805 ± 164550 ± 72.2 ± 0.572 ± 45.712
SRI-2921316 ± 481 ± 3346 ± 5977 ± 389 ± 5143 ± 40.2 ± 0.094 ± 25.622
SRI-293389.0 ± 1.571 ± 2204 ± 4762 ± 356 ± 2152 ± 31.18 ± 0.3363 ± 4623
SRI-2955411 ± 171 ± 1179 ± 2778 ± 257 ± 1860 ± 30.98 ± 0.4659 ± 6516
SRI-295742.3 ± 0.468 ± 252 ± 1572 ± 423 ± 552 ± 2InactiveInactive1023
SRI-295774.4 ± 0.870 ± 290 ± 1571 ± 220 ± 556 ± 23.4 ± 1.265 ± 64.620
SRI-2977619 ± 469 ± 2229 ± 4371 ± 3106 ± 1961 ± 26.09 ± 0.9758 ± 3612
SRI-297797.3 ± 2.263 ± 3147 ± 6371 ± 642 ± 1251 ± 21.2 ± 0.283 ± 35.820
SRI-297867.1 ± 2.270 ± 3143 ± 6168 ± 749 ± 2744 ± 41.1 ± 0.1100 ± 36.920
SRI-2998213 ± 273 ± 2259 ± 4171 ± 254 ± 751 ± 12.46 ± 1.2147 ± 6420
SRI-2998311 ± 270 ± 2203 ± 7973 ± 635 ± 957 ± 21.29 ± 0.3455 ± 3319
SRI-299912.1 ± 0.368 ± 163 ± 969 ± 24.7 ± 0.651 ± 11.22 ± 1.1218 ± 4230
SRI-305039.2 ± 1.270 ± 198 ± 2365 ± 316 ± 555 ± 20.67 ± 0.3734 ± 4211
SRI-3050411 ± 270 ± 2426 ± 4970 ± 250 ± 1455 ± 30.97 ± 0.6547 ± 7539
SRI-3050718 ± 371 ± 2132 ± 1677 ± 228 ± 654 ± 24.80 ± 1.8162 ± 727
SRI-305089.3 ± 1.165 ± 169 ± 1876 ± 33.9 ± 0.456 ± 10.15 ± 0.0934 ± 30.48
SRI-3051312 ± 272 ± 2153 ± 5565 ± 483 ± 2859 ± 42.97 ± 1.0350 ± 4713
SRI-305176.0 ± 0.770 ± 195 ± 1270 ± 223 ± 354 ± 10.16 ± 0.0843 ± 4416
SRI-305228.8 ± 1.163 ± 186 ± 5540 ± 513 ± 635 ± 3InactiveInactive110
SRI-305244.8 ± 0.671 ± 144 ± 676 ± 28.7 ± 0.956 ± 12.36 ± 1.1752 ± 629
SRI-308105.6 ± 0.864 ± 160 ± 1069 ± 211 ± 351 ± 20.82 ± 0.3625 ± 2211
SRI-308266.1 ± 164 ± 288 ± 1581 ± 218 ± 456 ± 21.28 ± 0.4042 ± 3314
SRI-308270.5 ± 0.163 ± 221 ± 767 ± 33.2 ± 0.958 ± 31.99 ± 0.3379 ± 3642
SRI-308288.9 ± 1.660 ± 2144 ± 3065 ± 320 ± 550 ± 22.61 ± 1.1460 ± 7216
SRI-3083711 ± 161 ± 1300 ± 5675 ± 367 ± 855 ± 11.70 ± 0.6244 ± 4627
SRI-3094621 ± 370 ± 278 ± 1775 ± 335 ± 1159 ± 31.17 ± 0.3244 ± 324
SRI-310347.4 ± 1.169 ± 194 ± 2263 ± 325 ± 749 ± 2InactiveInactive313
SRI-310397.4 ± 274 ± 431 ± 771 ± 38.0 ± 2.858 ± 33.15 ± 1.1172 ± 714
SRI-310401.2 ± 0.169 ± 111 ± 470 ± 43.1 ± 0.754 ± 23.74 ± 1.1091 ± 739
SRI-3104311 ± 167 ± 147 ± 1067 ± 222 ± 551 ± 22.16 ± 0.9730 ± 324
SRI-311421.9 ± 0.372 ± 217 ± 461 ± 22.4 ± 0.448 ± 12.34 ± 0.4592 ± 41.39
SRI-311431.7 ± 0.169 ± 116 ± 569 ± 43.0 ± 0.651 ± 23.39 ± 1.9952 ± 81.89
Cocaine200 ± 19100 ± 2329 ± 22102 ± 2273 ± 2498 ± 20.28 ± 0.0397 ± 31.41.7
GBR129351.1 ± 0.1104 ± 3N.D.N.D.N.D.N.D.2.0 × 10−3 ± 0.08 × 10−3101 ± 0.9
  • N.D., not determined.