(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

Research output: Research - peer-reviewArticle

  • 16 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.

LanguageEnglish (US)
JournalEuropean Journal of Pharmacology
Volume380
Issue number1
DOIs
StatePublished - Sep 3 1999
Externally publishedYes

Fingerprint

delta Opioid Receptor
methyl-2',6'-dimethyltyrosinyltetrahydroisoquinoline-3-carboxylic acid
GTP-Binding Proteins
Cricetulus
Ovary
Complementary DNA
Membranes

Keywords

  • δ-Opioid receptor
  • G protein
  • Inverse agonist

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

(2S,3R)TMT-L-Tic-OH is a potent inverse agonist at the human δ-opioid receptor. / Hosohata, Keiko; Burkey, Thomas H.; Alfaro-Lopez, Josua; Hruby, Victor J.; Roeske, William R.; Yamamura, Henry I.

In: European Journal of Pharmacology, Vol. 380, No. 1, 03.09.1999.

Research output: Research - peer-reviewArticle

Hosohata, Keiko ; Burkey, Thomas H. ; Alfaro-Lopez, Josua ; Hruby, Victor J. ; Roeske, William R. ; Yamamura, Henry I./ (2S,3R)TMT-L-Tic-OH is a potent inverse agonist at the human δ-opioid receptor. In: European Journal of Pharmacology. 1999 ; Vol. 380, No. 1.
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AU - Hruby,Victor J.

AU - Roeske,William R.

AU - Yamamura,Henry I.

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