Table 4

Effect of hSERT/dSERT TMD II divergent residues on 7-BT species selectivity. [3H]5-HT transport assays were performed in hSERT, dSERT, D136, Y95F, or double mutant transiently transfected HeLa cells. The Y95F/TMD II double mutants were constructed as detailed under Experimental Procedures. K I values were determined from competition uptake assays in transiently transfected HeLa cells and are the results of at least three independent experiments. Results are presented as mean ± S.E.M.

Construct7-BT KI
μM
hSERT1.3  ± 0.1
dSERT0.32  ± 0.03
D1360.41  ± 0.03
hSERT Y95F0.17  ± 0.01
 L119V1.9  ± 0.6
 Y95F/L119V0.22  ± 0.03
 T122C1.5  ± 0.2
 Y95F/T122C0.13  ± 0.01
 I123L2.2  ± 0.5
 Y95F/I123L0.14  ± 0.07
 M124F2.0  ± 0.8
 Y95F/M124F0.08  ± 0.01
 A125L3.6  ± 0.14-a
 Y95F/A125L0.28  ± 0.014-b
 I130L1.1  ± 0.2
 Y95F/I130L0.11  ± 0.01

  • ↵4-a  Significantly greater than hSERT (p < 0.001).

  • ↵4-b  Significantly greater than Y95F (p < 0.001).