Functional [3H]5HT uptake inhibition analysis at hSERT WT and
hSERT S438T. A, upper, structure of inhibitors having one (R = H)
or two (R = CH3) methyl groups at the aminopropyl chain.
Lower, characterization of pairs of inhibitors having a single
(blue squares, WT; blue triangles, S438T) or two (▪,
WT; ▴, S438T) methyl groups at the aminopropyl chain. B,
graphical summary of observed fold change in Ki between WT
and S438T for each inhibitor pair (mean ± S.E.; n = 6-8).
Ki values and statistics are shown in
Table 1.