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, Frank Porreca

Research output: Contribution to journalArticle

3 Citations (Scopus)

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 - 1995

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Methionine Enkephalin
Morphine
Analgesics
Naloxone
Morphine Dependence
Tail
Water

Keywords

  • antinociception
  • met-enkephalin analogue
  • opioid
  • peptide
  • run agonist

ASJC Scopus subject areas

  • Pharmacology

Cite this

Novel met-enkephalin analogue : a potent systemic mu agonist antinociceptive agent. / Nath, C.; Patnaikt, G. K.; Haqt, W.; Mathur, K. B.; Srimal, R. C.; Dhawan, B. N.; Porreca, Frank.

In: Pharmacological Research, Vol. 31, No. 5, 1995, p. 269-273.

Research output: Contribution to journalArticle

Nath, C, Patnaikt, GK, Haqt, W, Mathur, KB, Srimal, RC, Dhawan, BN & Porreca, F 1995, 'Novel met-enkephalin analogue: a potent systemic mu agonist antinociceptive agent', Pharmacological Research, vol. 31, no. 5, pp. 269-273. https://doi.org/10.1016/1043-6618(95)80031-X
Nath, C. ; Patnaikt, G. K. ; Haqt, W. ; Mathur, K. B. ; Srimal, R. C. ; Dhawan, B. N. ; Porreca, Frank. / Novel met-enkephalin analogue : a potent systemic mu agonist antinociceptive agent. In: Pharmacological Research. 1995 ; Vol. 31, No. 5. pp. 269-273.
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