Relative efficacies of 6-opioid receptor agonists at the cloned human δ-opioid receptor

Raymond M. Quock, Yoshiaki Hosohata, Richard J. Knapp, Thomas H. Burkey, Keiko Hosohata, Xiaoyan Zhang, Kenner C. Rice, Hiroshi Nagase, Victor J. Hruby, Frank Porreca, William R. Roeske, Henry I. Yamamura

Research output: Contribution to journalArticle

30 Scopus citations

Abstract

The present study was conducted to determine the relative efficacies of the selective δ-opioid receptor agonists SNC80((+)-4-[(αR)-α-((2S,5R)-4-allyl-2,5-dimethyl-1- piperazinyl)-3- S,5 R) -4-allyl-2,5-dimethyl-1-piherazinyl)-3-methoxybenzyl]-N,N- diethylbenzamide), pCl-DPDPE (cyclic[D-Pen2,4'-ClPhe4,D-Pen5]enkephalin) and (-)-TAN67 ((-)-2-methyl-4aα-(3-hydroxyphenyl)-1,2,3,4,4a,5,12,12aα-octahyhro-quinolino -[2,3,3-g]isoquinoline). Experiments compared the abilities of the three drugs to competitively inhibit [3H]naltrindole binding and also stimulate [35S]GTPγS binding in membranes prepared from stably transfected Chinese hamster ovary (CHO) cells that express the cloned human δ-opioid receptor. Efficacy was determined according to the formula: efficacy = (E(max-A)/E(maxi))(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.

Original languageEnglish (US)
Pages (from-to)101-104
Number of pages4
JournalEuropean Journal of Pharmacology
Volume326
Issue number1
DOIs
StatePublished - May 12 1997

Keywords

  • Efficacy
  • Radioligand binding
  • [S]GTPγS binding
  • δ-Opioid receptor agonist
  • δ-Opioid receptor, human

ASJC Scopus subject areas

  • Pharmacology

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    Quock, R. M., Hosohata, Y., Knapp, R. J., Burkey, T. H., Hosohata, K., Zhang, X., Rice, K. C., Nagase, H., Hruby, V. J., Porreca, F., Roeske, W. R., & Yamamura, H. I. (1997). Relative efficacies of 6-opioid receptor agonists at the cloned human δ-opioid receptor. European Journal of Pharmacology, 326(1), 101-104. https://doi.org/10.1016/S0014-2999(97)83488-7