The dipeptidyl peptidase IV (CD26, EC 3.4.14.5) inhibitor vildagliptin is a potent antihyperalgesic in rats by promoting endomorphin-2 generation in the spinal cord

Kornél Király, Anne Marie Lambeir, Judit Szalai, Apolka Szentirmay, Walter Luyten, István Barna, Zita Puskár, Márk Kozsurek, András Z. Rónai

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

We have reported previously that the dipeptidyl peptidase IV inhibitor Ile-Pro-Ile had an antihyperalgesic action in rats when given intrathecally in the carrageenan-induced hyperalgesia, as detected by the Randall-Selitto test. Vildagliptin, a non-peptide inhibitor of the same enzyme, which is already on the market as an "euglycemic" agent in diabetics, has a slightly more potent and more sustained antihyperalgesic effect in the same test when given by the same route. The action of 3 nmol/rat vildagliptin could be antagonized by subcutaneous naltrexone (0.5 mg/kg) pretreatment, or by intrathecally co-administered specific antiserum to endomorphin-2. Thus, the antihyperalgesia by vildagliptin, similarly to Ile-Pro-Ile, was opioid receptor-mediated and could be attributed to the promotion of endomorphin-2 generation in rat spinal cord dorsal horn. Furthermore, vildagliptin (1 mg/kg) is a potent antihyperalgesic also when given subcutaneously.

Original languageEnglish
Pages (from-to)195-199
Number of pages5
JournalEuropean Journal of Pharmacology
Volume650
Issue number1
DOIs
Publication statusPublished - Jan 10 2011

Keywords

  • Antihyperalgesic effect
  • Carrageenan-induced hyperalgesia
  • Dipeptidyl peptidase IV
  • Endomorphin-2 generation
  • Vildagliptin

ASJC Scopus subject areas

  • Pharmacology

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