Related Experiment Video
Updated: Jul 13, 2026

A Plate-Based Assay for the Measurement of Endogenous Monoamine Release in Acute Brain Slices
Published on: August 11, 2021
Therapeutic doses of amphetamine and methylphenidate selectively redistribute the vesicular monoamine transporter-2
Evan L Riddle1, Glen R Hanson, Annette E Fleckenstein
1Department of Pharmacology and Toxicology, University of Utah, Salt Lake City, Utah 84112, USA. evan.riddle@pharm.utah.edu
Abstract:
High-dose administration of psychostimulants traffics the vesicular monoamine transporter-2 (VMAT-2), as assessed by subcellular fractionation of rat striatal tissue. This study demonstrates that administration of low doses of amphetamine or methylphenidate differentially traffic VMAT-2 within nerve terminals, with effects similar to those observed after high-dose administration. Trafficking of vesicular glutamate, acetylcholine, or GABA transporters was not altered by high-or low-dose amphetamine or methylphenidate treatment. These data represent the first report that amphetamine redistributes VMAT-2 protein. In addition, these data demonstrate that the trafficking of VMAT-2 after amphetamine or methylphenidate is selective for monoaminergic neurons.
Related Concept Videos
Adrenergic Agonists: Indirect-Acting Agents
One mechanism involves depleting stored catecholamines by displacing them from synaptic vesicles. These agents, known as "displacers," are transported into vesicles at the expense of noradrenaline. Examples include amphetamine and tyramine, which lack a catechol moiety, resulting in prolonged action, improved oral bioavailability, and...
Drugs Affecting Neurotransmitter Release or Uptake
Drugs Affecting Neurotransmitter Synthesis
Adrenergic Agonists: Mixed-Action Agents
Ephedrine and pseudoephedrine lack a catecholamine group, making them less susceptible to degradation by metabolic enzymes. They have increased oral bioavailability and lipophilicity, resulting in a longer duration of action. Their response is reduced by...
Antidepressant Drugs: MAOIs and Other Agents
Neurochemical Transmission: Sites of Drug Action

