Differential down-regulation of the human d-opioid receptor by SNC80 and [D-Pen2, D-Pen5]enkephalin

Takashi Okura; Scott M. Cowell; Eva Varga; Thomas H. Burkey; William R. Roeske; Victor J Hruby; Henry I. Yamamura

doi:10.1016/S0014-2999(99)00761-X

Differential down-regulation of the human d-opioid receptor by SNC80 and [D-Pen², D-Pen⁵]enkephalin

Takashi Okura, Scott M. Cowell, Eva Varga, Thomas H. Burkey, William R. Roeske, Victor J Hruby, Henry I. Yamamura

Research output: Contribution to journal › Article › peer-review

21 Scopus citations

Abstract

We examined the contribution of the human d-opioid receptor carboxyl terminal tail to (+)-4-[(aR)-a-((2S,5R)-4-allyl-2,5-dimethyl-1- piperazinyl)-3-methoxybenzyl]-N, N-diethylbenzamide (SNC80)- and cyclic[D- Pen², D-Pen⁵]enkephalin (DPDPE)-mediated receptor down-regulation. Both SNC80 and DPDPE mediated down-regulation of an epitope tagged human d-opioid receptor. Truncation of the human d-opioid receptor after Gly³³⁸ 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.

Original language	English (US)
Pages (from-to)	R11-R13
Journal	European Journal of Pharmacology
Volume	387
Issue number	2
DOIs	https://doi.org/10.1016/S0014-2999(99)00761-X
State	Published - Jan 10 2000

Keywords

Carboxyl terminal tail
Down-regulation
d-Opioid receptor

ASJC Scopus subject areas

Pharmacology

Access to Document

10.1016/S0014-2999(99)00761-X

Cite this

@article{063aefc3626444de86e8b849138176c1,

title = "Differential down-regulation of the human d-opioid receptor by SNC80 and [D-Pen2, D-Pen5]enkephalin",

abstract = "We examined the contribution of the human d-opioid receptor carboxyl terminal tail to (+)-4-[(aR)-a-((2S,5R)-4-allyl-2,5-dimethyl-1- piperazinyl)-3-methoxybenzyl]-N, N-diethylbenzamide (SNC80)- and cyclic[D- Pen2, D-Pen5]enkephalin (DPDPE)-mediated receptor down-regulation. Both SNC80 and DPDPE mediated down-regulation of an epitope tagged human d-opioid receptor. Truncation of the human d-opioid receptor after Gly338 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.",

keywords = "Carboxyl terminal tail, Down-regulation, d-Opioid receptor",

author = "Takashi Okura and Cowell, {Scott M.} and Eva Varga and Burkey, {Thomas H.} and Roeske, {William R.} and Hruby, {Victor J} and Yamamura, {Henry I.}",

note = "Funding Information: We thank Michelle Thatcher and Carol Haussler for their assistance with the maintenance of cell lines expressing the WT-myc-his and the Δ 34 -myc-his and Sue Waite for assistance. This work was supported in part by grants from the Arizona Disease Control Research Commission and NIDA.",

year = "2000",

month = jan,

day = "10",

doi = "10.1016/S0014-2999(99)00761-X",

language = "English (US)",

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pages = "R11--R13",

journal = "European Journal of Pharmacology",

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T1 - Differential down-regulation of the human d-opioid receptor by SNC80 and [D-Pen2, D-Pen5]enkephalin

AU - Okura, Takashi

AU - Cowell, Scott M.

AU - Varga, Eva

AU - Burkey, Thomas H.

AU - Roeske, William R.

AU - Hruby, Victor J

AU - Yamamura, Henry I.

N1 - Funding Information: We thank Michelle Thatcher and Carol Haussler for their assistance with the maintenance of cell lines expressing the WT-myc-his and the Δ 34 -myc-his and Sue Waite for assistance. This work was supported in part by grants from the Arizona Disease Control Research Commission and NIDA.

PY - 2000/1/10

Y1 - 2000/1/10

N2 - We examined the contribution of the human d-opioid receptor carboxyl terminal tail to (+)-4-[(aR)-a-((2S,5R)-4-allyl-2,5-dimethyl-1- piperazinyl)-3-methoxybenzyl]-N, N-diethylbenzamide (SNC80)- and cyclic[D- Pen2, D-Pen5]enkephalin (DPDPE)-mediated receptor down-regulation. Both SNC80 and DPDPE mediated down-regulation of an epitope tagged human d-opioid receptor. Truncation of the human d-opioid receptor after Gly338 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.

AB - We examined the contribution of the human d-opioid receptor carboxyl terminal tail to (+)-4-[(aR)-a-((2S,5R)-4-allyl-2,5-dimethyl-1- piperazinyl)-3-methoxybenzyl]-N, N-diethylbenzamide (SNC80)- and cyclic[D- Pen2, D-Pen5]enkephalin (DPDPE)-mediated receptor down-regulation. Both SNC80 and DPDPE mediated down-regulation of an epitope tagged human d-opioid receptor. Truncation of the human d-opioid receptor after Gly338 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.

KW - Carboxyl terminal tail

KW - Down-regulation

KW - d-Opioid receptor

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