ICI 154,129, a delta-opioid receptor antagonist raises seizure threshold in rats

Eur J Pharmacol. 1984 Jan 13;97(1-2):141-4. doi: 10.1016/0014-2999(84)90523-5.

Abstract

Acute i.c.v. administration of ICI 154,129 (100-600 micrograms), a delta-opioid receptor antagonist, raised the seizure threshold in a dose-related manner in rats exposed to flurothyl, a volatile convulsant. Pretreatment with naloxone or beta-funaltrexamine (beta-FNA) antagonized this effect. Lower doses of ICI 154,129 (12.5-50 micrograms), which did not influence seizure threshold, selectively antagonized the anticonvulsant action of [D-Ala2,D-Leu5]enkephalin (DADLE) in the same procedure. Consequently, it may be inferred that ICI 154,129 at high doses has mu-agonist and at low doses delta-antagonist properties in the rat flurothyl test.

MeSH terms

  • Animals
  • Enkephalin, Leucine / analogs & derivatives*
  • Enkephalin, Leucine / antagonists & inhibitors
  • Enkephalin, Leucine / pharmacology
  • Enkephalin, Leucine-2-Alanine
  • Male
  • Naloxone / pharmacology
  • Naltrexone / analogs & derivatives
  • Naltrexone / pharmacology
  • Narcotic Antagonists / pharmacology*
  • Rats
  • Rats, Inbred Strains
  • Receptors, Opioid / drug effects*
  • Seizures / drug therapy*

Substances

  • Narcotic Antagonists
  • Receptors, Opioid
  • Naloxone
  • Enkephalin, Leucine
  • Naltrexone
  • Enkephalin, Leucine-2-Alanine
  • beta-funaltrexamine
  • ICI 154129