Clinically relevant doses of methylphenidate significantly occupy norepinephrine transporters in humans in vivo.

ABSTRACT:

Background

Attention-deficit/hyperactivity disorder is a psychiatric disorder that starts in childhood. The mechanism of action of methylphenidate, the most common treatment for attention deficit hyperactivity disorder, is unclear. In vitro, the affinity of methylphenidate for the norepinephrine transporter (NET) is higher than that for the dopamine transporter (DAT). The goal of this study was to use positron emission tomography to measure the occupancy of brain norepinephrine transporter by methylphenidate in vivo in humans.

Methods

We used (S,S)-[¹¹C] methylreboxetine ([¹¹C]MRB) to determine the effective dose 50 (ED₅₀) of methylphenidate for NET. In a within-subject design, healthy subjects (n = 11) received oral, single-blind placebo and 2.5, 10, and 40 mg of methylphen

SUBMITTER: Hannestad J 

PROVIDER: S-EPMC3742016 | biostudies-literature | 2010 Nov

REPOSITORIES: biostudies-literature