TABLE 1

Inhibition of monoamine transporter binding in vitro by TAS-303 and duloxetine

The affinity of each compound was measured by the inhibition of [125I]RTI-55 binding for NET and DAT, and [3H]paroxetine binding for SERT to respective membranes. Ki values for receptor binding were determined from three independent experiments using seven drug concentrations. Results are shown as the mean ± S.E.M.

CompoundMonoamine Transporter Binding KiSelectivity
NETSERTDATSERT/NETDAT/NET
nM
TAS-30350.9 ± 1.91560 ± 771290 ± 6931253
Duloxetine3.42 ± 0.250.283 ± 0.033157 ± 70.0846