sigma(2) Receptors regulate changes in sphingolipid levels in breast tumor cells

Eur J Pharmacol. 2002 May 17;443(1-3):207-9. doi: 10.1016/s0014-2999(02)01581-9.

Abstract

sigma(2) Receptors induce apoptosis in various cell types. The sphingolipid, ceramide as well as the sphingoid bases are involved in cell proliferation. Sphingolipids of MCF-7/Adr- and T47D breast tumor cells were metabolically radiolabeled. The sigma(2) receptor agonists (+)-1R,5R-E-8-(3,4-dichlorobenzylidene)-5-(3-hydroxyphenyl)-2-methylmorphan-7-one (CB-184) and 1S,2R-(--)-cis-N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)-cyclohexylamine (BD737) caused dose-dependent increases in [(3)H]ceramide, with concomitant decreases in [(3)H]sphingomyelin. Both effects were attenuated by the novel sigma(2) receptor antagonist, N-phenethylpiperidine oxalate (AC927). sigma(2) Receptors may produce effects on cell growth and apoptosis by regulating the sphingolipid pathway.

Publication types

  • Comparative Study

MeSH terms

  • Benzylidene Compounds / pharmacology
  • Breast Neoplasms
  • Cell Division
  • Cyclohexylamines / pharmacology
  • Humans
  • Infant
  • Morphinans / pharmacology
  • Oxalates / pharmacology
  • Piperidines / pharmacology
  • Pyrrolidines / pharmacology
  • Receptors, sigma / agonists
  • Receptors, sigma / physiology*
  • Sphingomyelins / metabolism*
  • Tumor Cells, Cultured

Substances

  • Benzylidene Compounds
  • CB 182
  • Cyclohexylamines
  • Morphinans
  • N-phenethylpiperidine oxalate
  • Oxalates
  • Piperidines
  • Pyrrolidines
  • Receptors, sigma
  • Sphingomyelins
  • BD 737