Mutation S363A in the human δ-opioid receptor selectively reduces down-regulation by a peptide agonist

Edita Navratilova, Eva V. Varga, Dagmar Stropova, Janelle C. Jambrosic, William R. Roeske, Henry I. Yamamura

Research output: Contribution to journalArticle

4 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)341-343
Number of pages3
JournalEuropean Journal of Pharmacology
Volume485
Issue number1-3
DOIs
StatePublished - Feb 6 2004

Keywords

  • Down-regulation
  • Trafficking, agonist-directed
  • δ-Opioid receptor

ASJC Scopus subject areas

  • Pharmacology

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