. Author manuscript; available in PMC: 2010 Jun 1.

Published in final edited form as: Nat Struct Mol Biol. 2009 May 10;16(6):652–657. doi: 10.1038/nsmb.1602

Table 1.

Inhibition of [³H]serotonin uptake into HEK-293 cells expressing SERT mutants by SSRIs

Mutation	Sertraline (%)^a	R-fluoxetine (%)^a	S-fluoxetine (%)^a
Wild-type	99.7 ± 15.7	100 ± 13	100 ± 15
Ile108Leu	17,946 ± 5,944 **	89.5 ± 14.34	63.0 ± 13.1
Tyr175Glu	880 ± 333 **	175 ± 21	154 ± 25
Ile179Ala	31,057 ± 17,095 **	660 ± 372 **	1,130 ± 424 **
Ile179Phe	108,105 ± 28,821 **	72.1 ± 36.7	152 ± 28
Ile179Asp	50,319 ± 12,464 **	818 ± 263 **	2,042 ± 793 **
ΔAla401	20,944 ± 3,537 **	75.0 ± 17.5	154 ± 72
Val489Phe	272 ± 29.5 *	87.0 ± 11.3	103 ± 20
Val489Leu	1,654 ± 348 **	114 ± 21	38.2 ± 12.9
Lys490Thr	9,796 ± 2,449 **	112 ± 22	45.3 ± 10.4
Glu493Asp	250 ± 53.6 *	188 ± 29	59.0 ± 25.2
Glu493Gln	1,537 ± 371 **	334 ± 110 **	73.1 ± 34.6

Note:

Data are IC₅₀ values expressed as % of wild-type, shown as mean ± SEM of at least three experiments. The significance of measurements are indicated by * (P ≤ 0.05) and ** (P ≤ 0.005) compared with the wild-type (one-way analysis of variance, followed by the Holm-Sidak multiple comparisons test).