Sigma (σ) receptors as potential therapeutic targets to mitigate psychostimulant effects.

Matsumoto RR, Nguyen L, Kaushal N, Robson MJ
Adv Pharmacol. 2014 69: 323-86

PMID: 24484982 · DOI:10.1016/B978-0-12-420118-7.00009-3

Many psychostimulants, including cocaine and methamphetamine, interact with sigma (σ) receptors at physiologically relevant concentrations. The potential therapeutic relevance of this interaction is underscored by the ability to selectively target σ receptors to mitigate many behavioral and physiological effects of psychostimulants in animal and cell-based model systems. This chapter begins with an overview of these enigmatic proteins. Provocative preclinical data showing that σ ligands modulate an array of cocaine and methamphetamine effects are summarized, along with emerging areas of research. Together, the literature suggests targeting of σ receptors as an innovative option for combating undesired actions of psychostimulants through both neuronal and glial mechanisms.

© 2014 Elsevier Inc. All rights reserved.

MeSH Terms (11)

Animals Central Nervous System Stimulants Clinical Trials as Topic Cocaine Drug Delivery Systems Humans Methamphetamine Opipramol Protein Binding Receptors, sigma Substance-Related Disorders

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