Agonists at the δ-opioid receptor modify the binding of µ-receptor agonists to the µ-δ receptor hetero-oligomer.

ABSTRACT:

Background and purpose

µ- and δ-opioid receptors form heteromeric complexes with unique ligand binding and G protein-coupling profiles linked to G protein α z-subunit (Gα(z) ) activation. However, the mechanism of action of agonists and their regulation of the µ-δ receptor heteromer are not well understood.

Experimental approach

Competition radioligand binding, cell surface receptor internalization in intact cells, confocal microscopy and receptor immunofluorescence techniques were employed to study the regulation of the µ-δ receptor heteromer in heterologous cells with and without agonist exposure.

Key results

Gα(z) enhanced affinity of some agonists at µ-δ receptor heteromers, independent of agonist chemical structure. δ-Opioid agonists displaced µ-agonist binding w

SUBMITTER: Kabli N 

PROVIDER: S-EPMC2998692 | biostudies-literature | 2010 Nov

REPOSITORIES: biostudies-literature