(2S,3R)TMT-L-Tic-OH is a potent inverse agonist at the human δ-opioid receptor

Keiko Hosohata; Thomas H. Burkey; Josua Alfaro-Lopez; Victor J. Hruby; William R. Roeske; Henry I. Yamamura

doi:10.1016/S0014-2999(99)00516-6

(2S,3R)TMT-L-Tic-OH is a potent inverse agonist at the human δ-opioid receptor

Keiko Hosohata, Thomas H. Burkey, Josua Alfaro-Lopez, Victor J. Hruby, William R. Roeske, Henry I. Yamamura

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21 Scopus citations

Abstract

We examined the pharmacologic effect of β-methyl-2',6'-dimethyltyrosine-L-tetrahydroisoquinoline-3-carboxylic acid ((2S,3R)TMT-L-Tic-OH) on G protein activation in membranes prepared from Chinese Hamster Ovary cells transfected with cDNA of the human δ-opioid receptor. (2S,3R)TMT-L-Tic-OH inhibited G protein activation to 58% of basal with an EC₅₀ of 0.72 nM as determined by [³⁵S]GTPγS binding. These findings suggest that (2S,3R)TMT-L-Tic-OH is a highly potent inverse agonist at the human δ-opioid receptor. Copyright (C) 1999 Elsevier Science B.V.

Original language	English (US)
Pages (from-to)	R9-R10
Journal	European Journal of Pharmacology
Volume	380
Issue number	1
DOIs	https://doi.org/10.1016/S0014-2999(99)00516-6
State	Published - Sep 3 1999

Keywords

G protein
Inverse agonist
δ-Opioid receptor

ASJC Scopus subject areas

Pharmacology

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10.1016/S0014-2999(99)00516-6

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title = "(2S,3R)TMT-L-Tic-OH is a potent inverse agonist at the human δ-opioid receptor",

abstract = "We examined the pharmacologic effect of β-methyl-2',6'-dimethyltyrosine-L-tetrahydroisoquinoline-3-carboxylic acid ((2S,3R)TMT-L-Tic-OH) on G protein activation in membranes prepared from Chinese Hamster Ovary cells transfected with cDNA of the human δ-opioid receptor. (2S,3R)TMT-L-Tic-OH inhibited G protein activation to 58% of basal with an EC50 of 0.72 nM as determined by [35S]GTPγS binding. These findings suggest that (2S,3R)TMT-L-Tic-OH is a highly potent inverse agonist at the human δ-opioid receptor. Copyright (C) 1999 Elsevier Science B.V.",

keywords = "G protein, Inverse agonist, δ-Opioid receptor",

author = "Keiko Hosohata and Burkey, {Thomas H.} and Josua Alfaro-Lopez and Hruby, {Victor J.} and Roeske, {William R.} and Yamamura, {Henry I.}",

note = "Funding Information: The authors wish to thank Carol Haussler and Michelle Thatcher for their assistance with the maintenance of the hDOR/CHO cell line. These studies were supported by grants from NIDA and the Arizona Disease Control Research Commission.",

year = "1999",

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doi = "10.1016/S0014-2999(99)00516-6",

language = "English (US)",

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T1 - (2S,3R)TMT-L-Tic-OH is a potent inverse agonist at the human δ-opioid receptor

AU - Hosohata, Keiko

AU - Burkey, Thomas H.

AU - Alfaro-Lopez, Josua

AU - Hruby, Victor J.

AU - Roeske, William R.

AU - Yamamura, Henry I.

N1 - Funding Information: The authors wish to thank Carol Haussler and Michelle Thatcher for their assistance with the maintenance of the hDOR/CHO cell line. These studies were supported by grants from NIDA and the Arizona Disease Control Research Commission.

PY - 1999/9/3

Y1 - 1999/9/3

N2 - We examined the pharmacologic effect of β-methyl-2',6'-dimethyltyrosine-L-tetrahydroisoquinoline-3-carboxylic acid ((2S,3R)TMT-L-Tic-OH) on G protein activation in membranes prepared from Chinese Hamster Ovary cells transfected with cDNA of the human δ-opioid receptor. (2S,3R)TMT-L-Tic-OH inhibited G protein activation to 58% of basal with an EC50 of 0.72 nM as determined by [35S]GTPγS binding. These findings suggest that (2S,3R)TMT-L-Tic-OH is a highly potent inverse agonist at the human δ-opioid receptor. Copyright (C) 1999 Elsevier Science B.V.

AB - We examined the pharmacologic effect of β-methyl-2',6'-dimethyltyrosine-L-tetrahydroisoquinoline-3-carboxylic acid ((2S,3R)TMT-L-Tic-OH) on G protein activation in membranes prepared from Chinese Hamster Ovary cells transfected with cDNA of the human δ-opioid receptor. (2S,3R)TMT-L-Tic-OH inhibited G protein activation to 58% of basal with an EC50 of 0.72 nM as determined by [35S]GTPγS binding. These findings suggest that (2S,3R)TMT-L-Tic-OH is a highly potent inverse agonist at the human δ-opioid receptor. Copyright (C) 1999 Elsevier Science B.V.

KW - G protein

KW - Inverse agonist

KW - δ-Opioid receptor

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DO - 10.1016/S0014-2999(99)00516-6

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AN - SCOPUS:0032831431

VL - 380

SP - R9-R10

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

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ER -

(2S,3R)TMT-L-Tic-OH is a potent inverse agonist at the human δ-opioid receptor

Abstract

Keywords

ASJC Scopus subject areas

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