Voprosy meditsinskoi khimii (ISSN 0042-8809)

SeARCH FOR ENDOGENOUS SIGMA-RECEPTOR LIGAND

   
Samovilova N.N., Prokazova N.V.
PubMed Id: 8553633
Year: 1995 vol: 41  issue:5  pages: 9-13
Abstract: Whether there is an endogenous ligand for sigma receptors remains unknown. A total lipid fraction was isolated from the porcine liver, which was then subjected to chromatographic separation, yielding nine chromatographic fractions eluated at various chloroform/methanol ratios: each fraction was tested for its capacity of inhibiting the binding of (+)-[3H]SKF 10047 to hepatic sigma-receptors. The chromatographic fraction 7 + 7A (eluated at chloroform/methanol ratios of 60:40-10:90) which consisted mainly of phospholipids was found to have the highest activity. However, a complex analysis of this fraction revealed no relationship of its sigma-inhibiting activity to phospholipids. It is suggested that the non-competitive inhibition of (+)-[3H]SKF 10047 binding by the isolated active fraction is due to its presence of an endogenous ligand which, interacting with sigma-2 receptor, allosterically inhibits the binding of the labelled (+)-benzomorphan.
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Reference: Samovilova N.N., Prokazova N.V., SeARCH FOR ENDOGENOUS SIGMA-RECEPTOR LIGAND, Voprosy meditsinskoi khimii, 1995, vol: 41(5), 9-13.
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