Novel met-enkephalin analogue: A potent systemic mu agonist antinociceptive agent

C. Nath, G. K. Patnaikt, W. Haqt, K. B. Mathur, R. C. Srimal, B. N. Dhawan, F. Porreca

Research output: Contribution to journalArticle

3 Scopus citations

Abstract

A new met-enkephalin analogue (compound 82/205) was evaluated for its opioidergic activity in mice. The compound showed antinociception (warm water tail-flick test), tolerance, cross tolerance to morphine and physical dependence. The time course of antinociptive effect of the compound was comparable to morphine. The antinociceptive ED50 (μmol kg-1 i.p.) values for the compound and morphine base were 5.31 and 7.59, respectively. Its antinociceptive effect was blocked by naloxone, β-FNA (mu antagonist) and naloxonazine (mu1 antagonist) but not by ICI 174,864 (delta antagonist). Naloxone precipitated withdrawal jumpings were 2.6 times less in compound 82/205 treated mice than the morphine treated group. The new analogue compound 82/205 is a potent mu agonist antinociceptive with a possible weak dependence liability.

Original languageEnglish (US)
Pages (from-to)269-273
Number of pages5
JournalPharmacological Research
Volume31
Issue number5
DOIs
StatePublished - Jan 1 1995

Keywords

  • Antinociception
  • Met-enkephalin analogue
  • Opioid
  • Peptide
  • Run agonist

ASJC Scopus subject areas

  • Pharmacology

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