Relative efficacies of delta-opioid receptor agonists at the cloned human delta-opioid receptor

Eur J Pharmacol. 1997 May 12;326(1):101-4. doi: 10.1016/s0014-2999(97)83488-7.

Abstract

The present study was conducted to determine the relative efficacies of the selective delta-opioid receptor agonists SNC80 ((+)-4-[(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl )-3-methoxybenzyl]-N,N-diethylbenzamide), pCl-DPDPE (cyclic[D-Pen2,4'-ClPhe4,D-Pen5]enkephalin) and (-)-TAN67 ((-)-2-methyl-4a alpha-(3-hydroxyphenyl)-1,2,3,4,4a,5,12,12a alpha-octahydro-quinolino-[2,3,3-g]isoquinoline). Experiments compared the abilities of the three drugs to competitively inhibit [3H]naltrindole binding and also stimulate [35S]GTPgammaS binding in membranes prepared from stably transfected Chinese hamster ovary (CHO) cells that express the cloned human delta-opioid receptor. Efficacy was determined according to the formula: efficacy = (E(max-A)/Emax)(A'/A + 1) X 0.5. Results show that SNC80 and pCl-DPDPE had efficacy values that were about 6-7 times greater than that of (-)-TAN67.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzamides / pharmacology
  • CHO Cells
  • Cloning, Molecular
  • Cricetinae
  • Enkephalin, D-Penicillamine (2,5)-
  • Enkephalins / pharmacology
  • Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
  • Humans
  • Naltrexone / analogs & derivatives
  • Naltrexone / metabolism
  • Narcotic Antagonists / metabolism
  • Piperazines / pharmacology
  • Quinolines / pharmacology
  • Receptors, Opioid, delta / agonists*
  • Sulfur Radioisotopes

Substances

  • Benzamides
  • Enkephalins
  • Narcotic Antagonists
  • Piperazines
  • Quinolines
  • Receptors, Opioid, delta
  • Sulfur Radioisotopes
  • TAN 67
  • 4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamide
  • Guanosine 5'-O-(3-Thiotriphosphate)
  • Naltrexone
  • Enkephalin, D-Penicillamine (2,5)-
  • naltrindole