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Author Notes:

Leonard L. Howell,Yerkes National Primate Research Center, Emory University, Atlanta, Georgia, USA, lhowell@emory.edu

The authors would like to thank Susan Marshall for technical assistance in preparation of the manuscript.

The authors have no conflicts of interest to declare.


Research Funding:

Supported by Office of Research Infrastructure Programs/OD P51OD11132 (LLH); DA 031246 (LLH); and DA026946 (SSN)


  • Amphetamine
  • Cocaine
  • Dopamine
  • Drug discrimination
  • Monoamines
  • Neuroimaging
  • Nonhuman primates
  • Norepinephrine
  • Self-administration
  • Serotonin
  • Animals
  • Central Nervous System Stimulants
  • Citalopram
  • Cocaine-Related Disorders
  • Dose-Response Relationship, Drug
  • Humans
  • Membrane Transport Proteins
  • Morpholines
  • Substance-Related Disorders
  • Substrate Specificity
  • Treatment Outcome
  • Vesicular Monoamine Transport Proteins

Monoamine transporter inhibitors and substrates as treatments for stimulant abuse


Journal Title:

Advances in Pharmacological Sciences


Volume 69


, Pages 129-176

Type of Work:

Article | Post-print: After Peer Review


The acute and chronic effects of abused psychostimulants on monoamine transporters and associated neurobiology have encouraged development of candidate medications that target these transporters. Monoamine transporters, in general, and dopamine transporters, in particular, are critical molecular targets that mediate abuse-related effects of psychostimulants such as cocaine and amphetamine. Moreover, chronic administration of psychostimulants can cause enduring changes in neurobiology reflected in dysregulation of monoamine neurochemistry and behavior. The current review will evaluate evidence for the efficacy of monoamine transporter inhibitors and substrates to reduce abuse-related effects of stimulants in preclinical assays of stimulant self-administration, drug discrimination, and reinstatement. In considering deployment of monoamine transport inhibitors and substrates as agonist-type medications to treat stimulant abuse, the safety and abuse liability of the medications are an obvious concern, and this will also be addressed. Future directions in drug discovery should identify novel medications that retain efficacy to decrease stimulant use but possess lower abuse liability and evaluate the degree to which efficacious medications can attenuate or reverse neurobiological effects of chronic stimulant use.

Copyright information:

© 2014 Elsevier Inc. All rights reserved.

This is an Open Access work distributed under the terms of the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License (http://creativecommons.org/licenses/by-nc-nd/4.0/).

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