Agonist-specific regulation of the δ-opioid receptor

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

Research output: Contribution to journalReview articlepeer-review

40 Scopus citations


Delta opioid receptor (DOR) agonists are attractive potential analgesics, since these compounds exhibit strong antinociceptive activity with relatively few side effects. In the past decade, several novel classes of δ-opioid agonists have been synthesized. Recent experimental data indicate that structurally distinct opioid agonists interact differently with the δ-opioid receptor. Consequently, individual agonist-bound DOR conformations may interact differently with intracellular proteins. In the present paper, after a brief review of the cellular processes that contribute to homologous desensitization of the DOR signaling, we shall focus on experimental data demonstrating that chemically different agonists differ in their ability to phosphorylate, internalize, and/or down-regulate the DOR. Homologous regulation of the opioid receptor signaling is thought to play an important role in the development of opioid tolerance. Therefore, agonist-specific differences in DOR regulation suggest that by further chemical modification, δ-selective opioid analgesics can be designed that exhibit a reduced propensity for analgesic tolerance.

Original languageEnglish (US)
Pages (from-to)599-612
Number of pages14
JournalLife Sciences
Issue number6
StatePublished - Dec 24 2004


  • Agonist-directed trafficking
  • Delta opioid receptor
  • Down-regulation
  • Homologous regulation
  • Internalization
  • Receptor desensitization

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)


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