Cited by 131Parkinson's Disease Mechanisms and TreatmentsNeurotransmitter Receptor Influence on BehaviorNeuroscience and Neuropharmacology Research

Vesicular monoamine transporter 2: Role as a novel target for drug development

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Zheng, Guangrong, Dwoskin, Linda P., Crooks, Peter A.·2006·The AAPS Journal

Abstract

In the central nervous system, vesicular monoamine transporter 2 (VMAT2) is the only transporter that moves cytoplasmic dopamine (DA) into synaptic vesicles for storage and subsequent exocytotic release. Pharmacologically enhancing DA sequestration by VMAT2, and thus preventing the oxidation of DA in the cytoplasm, may be a strategy for treating diseases such as Parkinson's disease. VMAT2 may also be a novel target for the development of treatments for psychostimulant abuse. This review summarizes the possible role of VMAT2 as a therapeutic target, VMAT2 ligands reported in the literature, and the structure-activity relationship of these ligands, including tetrabenazine analogs, ketanserin analogs, lobeline analogs, and 3-amine-2-phenylpropene analogs. The molecular structure of VMAT2 and its relevance to ligand binding are briefly discussed.

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Authors
Zheng, G., Dwoskin, L. P., & Crooks, P. A.
Affiliations
University of Kentucky (US)
Corresponding author
Crooks, Peter A.
Venue
The AAPS Journal
Published
2006-12
Volume
8
Issue
4
Pages
E682-E692
ISSN
1550-7416 (ISSN-L)
OpenAlex
W2038763233
Cited by
125
References
131
Citations by year
2026: 2 · 2025: 3 · 2024: 8 · 2023: 2 · 2022: 3 · 2021: 3 · 2020: 1 · 2019: 3 · 2018: 8 · 2017: 5 · 2016: 6 · 2015: 7 · 2014: 10 · 2013: 9 · 2012: 11
FWCI
1.19
Type
journal article
Language
en
Open access
Locations
  • The AAPS Journal (publishedVersion)
  • PubMed Central (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • National Institutes of Health (DA 13519)
  • National Institute on Drug Abuse (DA 13519)
Topics
  • Health Sciences › Medicine › Neurology › Parkinson's Disease Mechanisms and Treatments
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Keywords
vesicular monoamine transporter 2, dopamine storage, synaptic vesicles, Parkinson's disease, stimulant abuse, structure-activity relationship, drug development
MeSH terms
Animals, Pharmaceutical Preparations, Humans, Ligands, Protein Binding, Drug Design, Drug Delivery Systems, Vesicular Monoamine Transport Proteins

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