The interaction of the two isomers of the opioid benzodiazepine tifluadom with μ-, δ-, and k-binding sites and their analgesic and intestinal effects in rats

P. Petrillo, M. Amato, A. Tavani

Research output: Contribution to journalArticlepeer-review

Abstract

The (+) and (-) isomers of tifluadom were assessed in rats for their opioid activities. In vitro (+)-tifluadom was almost equipotent at μ- and κ- sites and about 10 times less potent at δ-sites: (-)-tifluadom had the same binding spectrum but was 10-20 times less potent. In vivo (+)-tifluadom delayed the hot-plate reaction time; this effect was antagonized by naloxone, but not by Ro 15-1788. (-)-Tifluadom up to 20 mg/kg had no antinociceptive effect. In the intestinal transit test analgesic doses of (+)-tifluadom did not delay the intestinal transit of a charcoal meal in rats and had weak antagonist activity against morphine-induced inhibition of intestinal transit, whereas (-)-tifluadom had neither agonist nor antagonist effect. It thus appears that (+)-and (-)-tifluadom are not selective in vitro and in vivo for one type of opioid binding site/receptor.

Original languageEnglish
Pages (from-to)403-406
Number of pages4
JournalNeuropeptides
Volume5
Issue number4-6
DOIs
Publication statusPublished - 1985

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology
  • Endocrinology, Diabetes and Metabolism
  • Clinical Neurology
  • Neuroscience(all)
  • Cellular and Molecular Neuroscience

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