R-modafinil (armodafinil): a unique dopamine uptake inhibitor and potential medication for psychostimulant abuse.

ABSTRACT:

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 [(3)H] dopamine (DA) uptake and [(3)H]WIN 35428 binding in human dopamine transporter (DAT) wild-type and mutants with altered conformational equilibria. Data were compared with cocaine and the atypical DA uptake inhibitor, JHW 007. R- and S-modafinil were also evaluated in microdialysis studies in the mouse nucleus accumbens shell and in a cocaine discrimination procedure.

Results

(±)-, R-, and S-modafinil bind to the DAT and

SUBMITTER: Loland CJ 

PROVIDER: S-EPMC3413742 | biostudies-literature | 2012 Sep

REPOSITORIES: biostudies-literature