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

Neuropharmacology. 1984 Aug;23(8):983-7. doi: 10.1016/0028-3908(84)90015-7.

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. (+)-SKF-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.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Binding, Competitive
  • Brain / metabolism
  • Dihydromorphine / metabolism
  • Electroencephalography
  • Female
  • Hallucinogens*
  • Humans
  • Morphine / pharmacology
  • Morphine Dependence / physiopathology
  • Phenazocine / analogs & derivatives*
  • Phenazocine / pharmacology
  • Rats
  • Rats, Inbred Strains
  • Receptors, Opioid / drug effects*
  • Receptors, Opioid / physiology*
  • Receptors, sigma
  • Stereoisomerism

Substances

  • Hallucinogens
  • Receptors, Opioid
  • Receptors, sigma
  • SK&F 10047
  • Morphine
  • Dihydromorphine
  • Phenazocine