Differential down-regulation of the human delta-opioid receptor by SNC80 and [D-Pen(2),D-Pen(5)]enkephalin

Eur J Pharmacol. 2000 Jan 10;387(2):R11-3. doi: 10.1016/s0014-2999(99)00761-x.

Abstract

We examined the contribution of the human delta-opioid receptor carboxyl terminal tail to (+)-4-[(alphaR)-alpha-((2S,5R)-4-allyl-2, 5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide (SNC80)- and cyclic[D-Pen(2),D-Pen(5)]enkephalin (DPDPE)-mediated receptor down-regulation. Both SNC80 and DPDPE mediated down-regulation of an epitope tagged human delta-opioid receptor. Truncation of the human delta-opioid receptor after Gly(338) 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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Benzamides / pharmacology*
  • Down-Regulation
  • Enkephalin, D-Penicillamine (2,5)- / pharmacology*
  • Humans
  • Naltrexone / analogs & derivatives
  • Naltrexone / metabolism
  • Piperazines / pharmacology*
  • Receptors, Opioid, delta / chemistry
  • Receptors, Opioid, delta / drug effects*
  • Receptors, Opioid, delta / metabolism

Substances

  • Benzamides
  • Piperazines
  • Receptors, Opioid, delta
  • 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamide
  • Naltrexone
  • Enkephalin, D-Penicillamine (2,5)-
  • naltrindole