Down-regulation of super(3)H-lofentanil binding to opiate receptors in different cultured neuronal cells

There was stereospecific binding of super(3)H-lofentanil to membranes of neuroblastoma-glioma NG 108-15 cells which are known to bear high affinity binding sites for enkephalin derivatives ( delta -opiate receptor subtype). The specific binding of super(3)H-lofentanil to delta -opiate receptor subty...

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Published in:Naunyn-Schmiedeberg's archives of pharmacology 1989-01, Vol.339 (1-2), p.192-199
Main Authors: Maloteaux, J M, Octave, J N, Laterre, E C, Laduron, P M
Format: Article
Language:English
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Summary:There was stereospecific binding of super(3)H-lofentanil to membranes of neuroblastoma-glioma NG 108-15 cells which are known to bear high affinity binding sites for enkephalin derivatives ( delta -opiate receptor subtype). The specific binding of super(3)H-lofentanil to delta -opiate receptor subtype was down-regulated after prolonged incubation of the cells in the presence of leu- and met-enkephalin. The results strongly suggest specific binding of super(3)H-sufentanil and super(3)H-lofentanil mainly to the so-called mu -opiate receptors in cultured neurones and a specific binding of super(3)H-lofentanil to lower affinity delta -opiate receptors in neuroblastoma-glioma cells. The down-regulation of the mu -opiate binding sites in cultured neurones and that of the delta -site in neuroblastoma x glioma hybrid cells were dose- and temperature-dependent, induced by the corresponding high affinity agonists and prevented by naloxone.
ISSN:0028-1298