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Related Experiment Videos

Cocaine binding at sigma receptors.

J Sharkey1, K A Glen, S Wolfe

  • 1Neuroscience Branch, NIDA Addiction Research Center, Baltimore, MD 21224.

European Journal of Pharmacology
|April 27, 1988
PubMed
Summary

Cocaine and similar drugs may cause psychosis by interacting with sigma receptors. This interaction is supported by binding assay data and blood concentration levels in humans.

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Area of Science:

  • Neuroscience
  • Psychopharmacology

Background:

  • Cocaine and related psychostimulants are known to induce psychosis.
  • The precise neurobiological mechanisms underlying psychostimulant-induced psychosis are not fully understood.

Purpose of the Study:

  • To investigate the potential role of sigma receptors in the psychotomimetic effects of psychostimulants.
  • To examine the relationship between drug-receptor interactions and observed behavioral effects.

Main Methods:

  • Performed binding assays to determine the affinity (Ki values) of cocaine and related compounds for sigma receptors.
  • Correlated binding affinity with reported blood concentrations associated with psychosis in human volunteers.

Main Results:

  • Cocaine and related psychostimulants demonstrated significant interaction with sigma receptors in binding assays.
  • The measured Ki values were consistent with blood concentrations known to induce psychosis.

Conclusions:

  • The interaction of psychostimulants with sigma receptors is a plausible mechanism contributing to their psychotomimetic effects.
  • Sigma receptor modulation may represent a therapeutic target for managing psychostimulant-induced psychosis.

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