TABLE 2

Effects of modafinil on transporter binding and uptake inhibition in rat brain Transporter binding and uptake assays were conducted as described under Materials and Methods. Each value represents mean ± S.D. for three separate experiments.



Radioligand Binding Data

Uptake Inhibition Data

DAT KI
SERT Ki
NET Ki
DAT IC50
SERT IC50
NET IC50
nM
Modafinil 4800 ± 480 46,620 ± 8790 >92,000
GBR12909a 12.0 ± 1.9 105 ± 11 497 ± 17
Cocainea 187 ± 19 172 ± 15 3210 ± 149
Modafinil 4043 ± 385 >50,000 136,000 ± 13,900
GBR12909b 4.3 ± 0.3 73 ± 2 79 ± 5
Cocaineb



487 ± 25
304 ± 10
779 ± 30
  • a Binding data are reported in Rothman et al. (2008)

  • b Uptake inhibition data are reported in Rothman et al. (2001)