Chemically distinct opioid agonists have different abilities to down-regulate opioid receptors. The present study investigated the role of Ser363 in human δ-opioid receptor down-regulation by a δ-selective peptide- and non-peptide agonist. Cyclic[D-Pen 2,D-Pen5]enkephalin (DPDPE)-mediated down-regulation was significantly attenuated by a S363A mutation. In contrast, this mutation had no effect on down-regulation by (+)-4-[(αR)-α-((2S,5R)-4-allyl-2,5- dimethyl-1-piperazinyl)-3-methoxybenzyl]N,N-diethylbenzamide (SNC80). These results demonstrate that the molecular mechanism of the human δ-opioid receptor down-regulation is agonist-specific.
- Trafficking, agonist-directed
- δ-Opioid receptor
ASJC Scopus subject areas