Figure 4
From: Mechanism of Paroxetine (Paxil) Inhibition of the Serotonin Transporter
Potencies of SERT homologues & mutants for paroxetine, as assessed by (a–g) inhibition of 20 nM [3H]5-HT transport in transiently-transfected T-REx-293 cells or (h) inhibition of 0.2 nM [125I]RTI-55 binding to crude membranes prepared from transiently-transfected T-REx-293 cells. (a) Paroxetine inhibition of hsSERT-WT (
), dmSERT-WT (
), or ggSERT-WT (
). (b) Paroxetine inhibition of hsSERT-WT (
) versus hsSERT-I172M (
). (c) Paroxetine inhibition of dmSERT-WT (
) versus dmSERT-M167I (
). (d) Paroxetine inhibition of ggSERT-WT (
) versus ggSERT-V212I (
). (e) Paroxetine inhibition of hsSERT-WT (
) versus hsSERT-A169D (
). (f) Paroxetine inhibition of dmSERT-WT (
) versus dmSERT-D164A (
). (g) Paroxetine inhibition of ggSERT-WT (
) versus ggSERT-D209A (
). The blue arrows in panels e-g denote a decrease (panel e) or increase (panels f and g) of paroxetine potencies. (h) Paroxetine inhibition of [125I]RTI-55 binding to hsSERT-WT (
), hsSERT-A169D (
), or hsSERT-A169E (
). The blue arrow denotes a dramatic decrease in paroxetine binding affinity for both the hsSERT-A169D as well as the –A169E mutants relative to that for hsSERT-WT. The data in each panel represents a typical experiment, each performed in triplicate and repeated a minimum of 3 times (see Table 1). Data points and error bars represent the mean value with the standard error.
