Endomorphin-1 and endomorphin-2 are partial agonists at the human μ- opioid receptor

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

Research output: Contribution to journalArticle

58 Citations (Scopus)

Abstract

Recently two tetrapeptide ligands that bind preferentially to the μ- opioid receptor were identified and named endomorphin-1 and endomorphin-2. We examined the ability of these peptides to stimulate G protein activation in human μ-opioid receptor transfected B82 fibroblasts as measured by [35S]GTPγS binding to cell membranes. Both endomorphin-1 and -2 act as partial agonists in this assay system compared with the μ-selective agonist [D-Ala2,N-Me-Phe4, Gly-ol5]enkephalin (DAMGO). In addition, endomorphins demonstrate efficacy similar to morphine. These findings demonstrate that endomorphin peptides have similar activity at the μ-opioid receptor as morphine and suggest that these peptides have the potential to modulate neuronal activity in vivo.

Original languageEnglish (US)
Pages (from-to)111-114
Number of pages4
JournalEuropean Journal of Pharmacology
Volume346
Issue number1
DOIs
StatePublished - Apr 3 1998

Fingerprint

Opioid Receptors
Morphine
Peptides
Enkephalins
GTP-Binding Proteins
Fibroblasts
Cell Membrane
Ligands
endomorphin 1
endomorphin 2

Keywords

  • μ-Opioid receptor
  • Efficacy
  • Endomorphin-1
  • Endomorphin-2

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Endomorphin-1 and endomorphin-2 are partial agonists at the human μ- opioid receptor. / Hosohata, Keiko; Burkey, Thomas H.; Alfaro-Lopez, Josue; Varga, Eva; Hruby, Victor J; Roeske, William R; Yamamura, Henry I.

In: European Journal of Pharmacology, Vol. 346, No. 1, 03.04.1998, p. 111-114.

Research output: Contribution to journalArticle

Hosohata, Keiko ; Burkey, Thomas H. ; Alfaro-Lopez, Josue ; Varga, Eva ; Hruby, Victor J ; Roeske, William R ; Yamamura, Henry I. / Endomorphin-1 and endomorphin-2 are partial agonists at the human μ- opioid receptor. In: European Journal of Pharmacology. 1998 ; Vol. 346, No. 1. pp. 111-114.
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