σ2 Receptors regulate changes in sphingolipid levels in breast tumor cells

Keith W. Crawford; Andrew Coop; Wayne D. Bowen

doi:10.1016/S0014-2999(02)01581-9

σ₂ Receptors regulate changes in sphingolipid levels in breast tumor cells

Keith W. Crawford, Andrew Coop, Wayne D. Bowen

School of Medicine

Research output: Contribution to journal › Article › peer-review

75 Scopus citations

Abstract

σ₂ 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 σ₂ 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 [³H]ceramide, with concomitant decreases in [³H]sphingomyelin. Both effects were attenuated by the novel σ₂ receptor antagonist, N-phenethylpiperidine oxalate (AC927). σ₂ Receptors may produce effects on cell growth and apoptosis by regulating the sphingolipid pathway.

Original language	English (US)
Pages (from-to)	207-209
Number of pages	3
Journal	European Journal of Pharmacology
Volume	443
Issue number	1-3
DOIs	https://doi.org/10.1016/S0014-2999(02)01581-9
State	Published - May 17 2002

Keywords

Apoptosis
Ceramide
σ Receptor

ASJC Scopus subject areas

Pharmacology

Access to Document

10.1016/S0014-2999(02)01581-9

Cite this

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title = "σ2 Receptors regulate changes in sphingolipid levels in breast tumor cells",

abstract = "σ2 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 σ2 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 [3H]ceramide, with concomitant decreases in [3H]sphingomyelin. Both effects were attenuated by the novel σ2 receptor antagonist, N-phenethylpiperidine oxalate (AC927). σ2 Receptors may produce effects on cell growth and apoptosis by regulating the sphingolipid pathway.",

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AU - Coop, Andrew

AU - Bowen, Wayne D.

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N2 - σ2 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 σ2 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 [3H]ceramide, with concomitant decreases in [3H]sphingomyelin. Both effects were attenuated by the novel σ2 receptor antagonist, N-phenethylpiperidine oxalate (AC927). σ2 Receptors may produce effects on cell growth and apoptosis by regulating the sphingolipid pathway.

AB - σ2 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 σ2 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 [3H]ceramide, with concomitant decreases in [3H]sphingomyelin. Both effects were attenuated by the novel σ2 receptor antagonist, N-phenethylpiperidine oxalate (AC927). σ2 Receptors may produce effects on cell growth and apoptosis by regulating the sphingolipid pathway.

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