Analgesic and tolerance-inducing effects of the highly selective δ opioid agonist {A figure is presented} enkephalin in mice

G. Kovács, Noémi Nyolczas, Márta Kriván, K. Gulya

Research output: Contribution to journalArticle

20 Citations (Scopus)

Abstract

The novel and highly selective, conformationally restricted enkephalin analogue for δ-opioid receptors, {A figure is presented}enkephalin (DPDPE; Pen = penicillamine), was studied in various in vivo tests for analgesia, tolerance and physical dependence. Intracerebroventricular (i.c.v.) administration of DPDPE caused a dose-dependent, naloxone-reversible antinociception, measured with the heat-irradiant (tail-flick) method. Acute tolerance developed to the antinociceptive effect of DPDPE. DPDPE also caused mild signs of physical dependence (withdrawal hypothermia and body weight loss) after repeated peptide treatment. Severe signs of morphine withdrawal (e.g. withdrawal jumping) on the other hand, could not be reversed by the administration of DPDPE. It is concluded that the activation of central δ-opioid receptors may play a role in controlling pain mechanisms, and that this activation is followed by the rapid development of a tolerance to this action.

Original languageEnglish
Pages (from-to)347-353
Number of pages7
JournalEuropean Journal of Pharmacology
Volume150
Issue number3
DOIs
Publication statusPublished - Jun 10 1988

Fingerprint

D-Penicillamine (2,5)-Enkephalin
Enkephalins
Opioid Analgesics
Analgesics
Opioid Receptors
Penicillamine
Pain Measurement
Naloxone
Hypothermia
Morphine
Tail
Weight Loss
Hot Temperature
Body Weight
Pain
Peptides

Keywords

  • Analgesia
  • Physical dependence
  • Tolerance
  • δ Receptor agonists (selective)

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Analgesic and tolerance-inducing effects of the highly selective δ opioid agonist {A figure is presented} enkephalin in mice. / Kovács, G.; Nyolczas, Noémi; Kriván, Márta; Gulya, K.

In: European Journal of Pharmacology, Vol. 150, No. 3, 10.06.1988, p. 347-353.

Research output: Contribution to journalArticle

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