(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: Contribution to journalArticle

19 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 languageEnglish (US)
Pages (from-to)R9-R10
JournalEuropean Journal of Pharmacology
Volume380
Issue number1
DOIs
StatePublished - Sep 3 1999

Keywords

  • G protein
  • Inverse agonist
  • δ-Opioid receptor

ASJC Scopus subject areas

  • Pharmacology

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