Diprotin A, an inhibitor of dipeptidyl aminopeptidase IV(EC 3.4.14.5) produces naloxone - Reversible analgesia in rats

András Z. Rónai, Julianna Timár, Éva Makó, Franciska Erdo, Zsuzsanna Gyarmati, Géza Tóth, György Orosz, Susanne Fürst, József I. Székely

Research output: Contribution to journalArticle

37 Citations (Scopus)

Abstract

The dipeptidyl aminopeptidase IV (DP IV) inhibitor Diprotin A produces a full, dose-dependent, short-lasting and naloxone-reversible analgesia in the rat tail-flick test when given intracerebroventricularly, with an ED50 of 295 nmol/rat but it has no direct opioid agonist activity in the longitudinal muscle strip of guinea-pig ileum bioassay. Two of the potential DP IV substrates, morphiceptin and endomorphin 1, identified recently in bovine brain were also analgesic given by similar route. The action of endomorphin 1 was more potent (ED50 = 7.9 nmol/rat) and slightly but significantly more sustained than that of Diprotin A. Diprotin A neither potentiated nor prolonged the effect of a marginally analgesic dose of endomorphin 1. The distinct time course and the lack of potentiation indicate that in the analgesic effect of Diprotin A in rats the protection of a brain Tyr-Pro- peptide other than endomorphin 1 is involved.

Original languageEnglish
Pages (from-to)145-152
Number of pages8
JournalLife sciences
Volume64
Issue number2
DOIs
Publication statusPublished - Dec 4 1998

Keywords

  • Diprotin A
  • Endomorphins
  • Guinea-pig ileum
  • Mouse vas deferens
  • Opioid analgesia
  • Tyr-Pro-peptides

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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