Up-regulation of rat cortical σ receptors after subchronic administration of rimcazole and 1,3-di(2-tolyl)guanidine

D. T. Manallack, P. M. Beart

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The effects of subchronic administration of rimcazole and 1,3-di(2-tolyl)guanidine (DTG) on the central R(+)[3H]-3-[3-hydroxyphenyl]-N-(1-propyl)piperidine (R(+)[3H]-3-PPP) binding site were investigated in the rat. Subchronic treatment with rimcazole was characterized by a 30% increase in the density and a two-fold decrease in the affinity of R(+)[3H]-3-PPP binding sites relative to saline-treated animals. DTG, a more potent σ ligand, produced a similar alteration to the affinity but a 130% increase in the density of R(+)[3H]-3-PPP binding sites. These data thus provide evidence for the functional involvement of σ receptors in the central nervous system.

Original languageEnglish
Pages (from-to)1201-1203
Number of pages3
Issue number11
Publication statusPublished - 1 Jan 1988
Externally publishedYes


  • 1,3-di(2-tolyl)guanidine (DTG)
  • Adaptation
  • biological
  • rat
  • Receptor
  • rimcazole
  • Sigma

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