Cocaine and Cerebral Sigma-1 Receptor Occupancy

J. R. Lever, D. K. Miller, S. Z. Lever

Research output: Chapter in Book/Report/Conference proceedingChapter

1 Scopus citations


Cocaine activates sigma-1 σ(1) receptors, which function as molecular chaperones for diverse proteins including ion channels and neurotransmitter receptors. Consequently, cocaineσ-1 receptor interactions modulate multiple signaling pathways that contribute to the behavioral effects, abuse liability, and toxicity of the drug. Interventions with small-molecule antagonists of σ1 receptors represent a promising approach for the pharmacotherapy of cocaine abuse. In this chapter, we summarize recent findings regarding occupancy of σ1 receptors by cocaine and other σ1 receptor ligands, and discuss the correlation of σ1 receptor occupancy by antagonist ligands with attenuation of cocaine's motor stimulatory effects in a mouse model.

Original languageEnglish (US)
Title of host publicationThe Neuroscience of Cocaine
Subtitle of host publicationMechanisms and Treatment
PublisherElsevier Inc.
Number of pages9
ISBN (Electronic)9780128037928
ISBN (Print)9780128037508
StatePublished - May 16 2017


  • Cocaine
  • Locomotor activity
  • Mouse
  • Occupancy
  • Sigma receptor
  • Substance abuse

ASJC Scopus subject areas

  • General Psychology


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