[Search for an endogenous ligand for sigma receptors].
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.
Samovilova
N N
NN
Prokazova
N V
NV
D000494:Allosteric Regulation; D000818:Animals; D001575:Benzomorphans / Q000378:metabolism; D002853:Chromatography, Liquid; D008024:Ligands; D050356:Lipid Metabolism; D008055:Lipids / Q000302:isolation & purification; D010620:Phenazocine / Q000031:analogs & derivatives* / Q000378:metabolism; D017480:Receptors, sigma / Q000378:metabolism*; D013552:Swine
D001575:Benzomorphans; D008024:Ligands; D008055:Lipids; D017480:Receptors, sigma; C012134:SK&F 10047; D010620:Phenazocine
Poisk éndogennogo liganda sigma-retseptorov.