Figure 3. Inhibition of [³H]5-HT transport and [³H]citalopram binding by paroxetine and the Br- and I-derivatives.

(a) 5-HT-transport of wild-type SERT and its inhibition by paroxetine, Br-, and I-paroxetine. Data are mean ± s.e.m. (n = 6). (b) Competition binding of paroxetine and its derivatives to ts2-inactive SERT. In panels a and b, paroxetine, Br-paroxetine, and I-paroxetine curves are shown as black, red, and blue lines, respectively. Data are mean ± s.e.m. (n = 6). (c) Competition binding of paroxetine to ts2-active (black), Asn177Val (red), Asn177Thr (green), and Asn177Gln (blue). Data are mean ± s.e.m. (n = 3). (d) Competition binding of Br-paroxetine. Data are mean ± s.e.m. (n = 3). (e) Competition binding of I-paroxetine. Data are mean ± s.e.m. (n = 3). The values associated with these experiments are reported in Tables 2 and 3.