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The σ Receptor

  • Chapter
The Opiate Receptors

Part of the book series: The Receptors ((REC))

Abstract

The psychotropic actions of opiates and opioid peptides are mediated by interaction with µ, δ, and κ opioid receptors and the related σ receptor. The µ receptor is operationally defined as the high-affinity site at which morphine-like opioids produce analgesia and other classical opioid effects. The δ receptor is operationally defined as the receptor that is found in peripheral tissues such as the mouse vas deferens (Lord et al., 1977) as well as in the CNS (Chang et al., 1979), and that exhibits a higher affinity for the naturally occurring enkephalins (shorter opioid peptides) than for morphine. The κ receptor is the receptor at which ketocyclazocine-like opioids produce analgesia as well as their unique ataxic and sedative effects (Gilbert and Martin, 1976; Martin et al., 1976). More recently it has been defined as a receptor highly selective for dynorphin, a 17-amino acid opioid peptide (Chavkin et al., 1982). Actions at all three of these sites are reversible by the specific opioid antagonist naloxone, with decreasing sensitivity going from µ to δ to κ receptors.

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  1. R. Suzanne Zukin
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  1. Memorial Sloan-Kettering Cancer Center and Cornell University Medical College, New York, New York, USA

    Gavril W. Pasternak

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Zukin, R.S., Zukin, S.R. (1988). The σ Receptor. In: Pasternak, G.W. (eds) The Opiate Receptors. The Receptors. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-60761-990-1_5

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  • DOI: https://doi.org/10.1007/978-1-60761-990-1_5

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