TY - JOUR
T1 - σ2 Receptors regulate changes in sphingolipid levels in breast tumor cells
AU - Crawford, Keith W.
AU - Coop, Andrew
AU - Bowen, Wayne D.
PY - 2002/5/17
Y1 - 2002/5/17
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.
KW - Apoptosis
KW - Ceramide
KW - σ Receptor
UR - http://www.scopus.com/inward/record.url?scp=0037123809&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0037123809&partnerID=8YFLogxK
U2 - 10.1016/S0014-2999(02)01581-9
DO - 10.1016/S0014-2999(02)01581-9
M3 - Article
C2 - 12044812
AN - SCOPUS:0037123809
SN - 0014-2999
VL - 443
SP - 207
EP - 209
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
IS - 1-3
ER -