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

doi:10.1016/S0014-2999(97)83488-7

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 journal › Article › peer-review

31 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 language	English (US)
Pages (from-to)	101-104
Number of pages	4
Journal	European Journal of Pharmacology
Volume	326
Issue number	1
DOIs	https://doi.org/10.1016/S0014-2999(97)83488-7
State	Published - 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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10.1016/S0014-2999(97)83488-7

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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 journal › Article › peer-review

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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title = "Relative efficacies of 6-opioid receptor agonists at the cloned human δ-opioid receptor",

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.",

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AU - Quock, Raymond M.

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AU - Burkey, Thomas H.

AU - Hosohata, Keiko

AU - Zhang, Xiaoyan

AU - Rice, Kenner C.

AU - Nagase, Hiroshi

AU - Hruby, Victor J.

AU - Porreca, Frank

AU - Roeske, William R.

AU - Yamamura, Henry I.

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AB - 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.

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

Abstract

Keywords

ASJC Scopus subject areas

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