Sigma receptors mediate the psychotomimetic effects of N-allylnormetazocine (SKF-10,047), but not its opioid agonistic-antagonistic properties

N. Khazan, G. A. Young, E. E. El-Fakany, O. Hong, D. Calligaro

Research output: Contribution to journalArticle

Abstract

Our present findings suggest that SKF-10,047, the prototype sigma agonist, has its opioid entity residing with its (-) isomer, while both Its (+) and (-) isomers possess psychotogenic properties similar to those produced by PCP. We found that (-)-SKF-10,047 blocks EEG and behavioral effects of morphine in the naive rat, precipitates withdrawal in morphine-dependent rats, produces physical dependence as evidenced by naloxone-induced withdrawal, and displaces [3H]dihydromorphine from brain homogenates. (+)-SKP-10,047 did not produce dependence upon chronic treatment, and it did not displace [3H]dihydromorphine from brain homogenates. Such pharmacodynamic dissociation with SKF-10,047 suggests an association of sigma receptors with psychogenic, but not opioid effects. The latter are most likely mediated by mu or kappa receptors.

Original languageEnglish (US)
Pages (from-to)983-987
Number of pages5
JournalNeuropharmacology
Volume23
Issue number8
DOIs
StatePublished - Aug 1984

ASJC Scopus subject areas

  • Pharmacology
  • Cellular and Molecular Neuroscience

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