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

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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

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naltrindole
Opioid Receptors
Cricetulus
Ovary
Membranes
Pharmaceutical Preparations
4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamide
Pen(2,5)-4-chloro-Phe(4)-enkephalin
Ala(2)-enkephalinamide-met
rebemide
isoquinoline

Keywords

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

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Quock, R. M., Hosohata, Y., Knapp, R. J., Burkey, T. H., Hosohata, K., Zhang, X., ... 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

Relative efficacies of 6-opioid receptor agonists at the cloned human δ-opioid receptor. / Quock, Raymond M.; Hosohata, Yoshiaki; Knapp, Richard J.; Burkey, Thomas H.; Hosohata, Keiko; Zhang, Xiaoyan; Rice, Kenner C.; Nagase, Hiroshi; Hruby, Victor J; Porreca, Frank; Roeske, William R; Yamamura, Henry I.

In: European Journal of Pharmacology, Vol. 326, No. 1, 12.05.1997, p. 101-104.

Research output: Contribution to journalArticle

Quock, RM, Hosohata, Y, Knapp, RJ, Burkey, TH, Hosohata, K, Zhang, X, Rice, KC, Nagase, H, Hruby, VJ, Porreca, F, Roeske, WR & Yamamura, HI 1997, 'Relative efficacies of 6-opioid receptor agonists at the cloned human δ-opioid receptor', European Journal of Pharmacology, vol. 326, no. 1, pp. 101-104. https://doi.org/10.1016/S0014-2999(97)83488-7
Quock, Raymond M. ; Hosohata, Yoshiaki ; Knapp, Richard J. ; Burkey, Thomas H. ; Hosohata, Keiko ; Zhang, Xiaoyan ; Rice, Kenner C. ; Nagase, Hiroshi ; Hruby, Victor J ; Porreca, Frank ; Roeske, William R ; Yamamura, Henry I. / Relative efficacies of 6-opioid receptor agonists at the cloned human δ-opioid receptor. In: European Journal of Pharmacology. 1997 ; Vol. 326, No. 1. pp. 101-104.
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