BACKGROUND:(±)-Modafinil has piqued interest as a treatment for attention-
deficit/hyperactivity disorder and stimulant dependence. The R-enantiomer of modafinil
might have unique pharmacological properties that should be further investigated.
METHODS:(±)-Modafinil and its R-(−)-and S-(+)-enantiomers were synthesized and tested
for inhibition of [3H] dopamine (DA) uptake and [3H] WIN 35428 binding in human dopamine
transporter (DAT) wild-type and mutants with altered conformational equilibria. Data were …