Table 1 Paroxetine Inhibition Constants for SERT Homologues and Mutants^a.

^aUnits are expressed in nM and represent the average ± SEM.
^bParoxetine concentration at which half of 20 nM [³H]5-HT transport is inhibited relative to a “0 nM paroxetine” control.
^cInhibition constant calculated from the corresponding IC₅₀ and SERT mutant Michaelis constant (K_m) via the Cheng-Prusoff equation⁷⁴. Note that the IC₅₀ and K_i for the respective SERT construct are approximately the same because the [³H]5-HT concentration employed in the inhibition assay was far below the corresponding K_m.
^dDifference in paroxetine potency between wild-type and mutant SERTs calculated by dividing the corresponding K_i values, except for ggSERT-V212I, in which case the corresponding IC₅₀ values were used. Positive and negative numbers refer to gain and loss of paroxetine potency in the mutant, respectively.
^eNumber of individual experiments, each performed in triplicate.
^fp values determined by Students unpaired t-test. Values less than 0.05 indicate a statistically significant difference between the mutant and the WT K_i or IC₅₀ values.

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