Affinity of naloxone and its quaternary analogue for avian central δ and μ opioid receptors

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12 Scopus citations

Abstract

Quaternary narcotic antagonists that are assumed not to penetrate the blood brain barrier following systemic administration are commonly used to distinguish between peripheral and central actions of opiates. In mammals, these antagonists have a lower affinity for opioid receptors than their tertiary parent compounds. The relative affinity of quaternary vs. tertiary antagonists either for opioid receptors in non mammalian species or for specific receptor subtypes has, however, not been determined. Using brain tissues from a passerine songbird (Junco hyemalis), we found the affinity of the quaternary antagonist, naloxone methiodide (Nal MI), for brain opioid receptors to be less than 10% that of Nal HCl. Further, Nal MI affinity for μ and δ receptors is 8.7% and 3.7%, respectively, that of Nal HCl. These results confirm that tertiary narcotic antagonist quaternization substantially reduces the affinity of these derivatives for central opioid receptors. They show that this reduction is receptor-type selective, and they extend previous reports demonstrating functional similarities between mammalian and non mammalian central opioid receptors.

Original languageEnglish (US)
Pages (from-to)276-279
Number of pages4
JournalBrain Research
Volume757
Issue number2
DOIs
StatePublished - May 23 1997
Externally publishedYes

Keywords

  • DAMGO
  • DPDPE
  • Delta receptor
  • Junco
  • Mu receptor
  • Naloxone
  • Opioid
  • Quaternary naloxone

ASJC Scopus subject areas

  • Neuroscience(all)
  • Molecular Biology
  • Clinical Neurology
  • Developmental Biology

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