Differential down-regulation of the human d-opioid receptor by SNC80 and [D-Pen2, D-Pen5]enkephalin

Takashi Okura, Scott M. Cowell, Eva Varga, Thomas H. Burkey, William R. Roeske, Victor J Hruby, Henry I. Yamamura

Research output: Contribution to journalArticlepeer-review

21 Scopus citations

Abstract

We examined the contribution of the human d-opioid receptor carboxyl terminal tail to (+)-4-[(aR)-a-((2S,5R)-4-allyl-2,5-dimethyl-1- piperazinyl)-3-methoxybenzyl]-N, N-diethylbenzamide (SNC80)- and cyclic[D- Pen2, D-Pen5]enkephalin (DPDPE)-mediated receptor down-regulation. Both SNC80 and DPDPE mediated down-regulation of an epitope tagged human d-opioid receptor. Truncation of the human d-opioid receptor after Gly338 blocked DPDPE-mediated down-regulation. However, SNC80 mediated significant down- regulation of the truncated receptor. These findings suggest that SNC80- mediated down-regulation involves receptor domains in addition to the carboxyl terminal tail.

Original languageEnglish (US)
Pages (from-to)R11-R13
JournalEuropean Journal of Pharmacology
Volume387
Issue number2
DOIs
StatePublished - Jan 10 2000

Keywords

  • Carboxyl terminal tail
  • Down-regulation
  • d-Opioid receptor

ASJC Scopus subject areas

  • Pharmacology

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