Publication
Title
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
Author
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 RandallSelitto 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.
Language
English
Source (journal)
European journal of pharmacology. - Amsterdam, 1967, currens
Publication
Amsterdam : North-Holland , 2011
ISSN
0014-2999 [print]
1879-0712 [online]
Volume/pages
650 :1 (2011) , p. 195-199
ISI
000285893800026
Full text (Publisher's DOI)
UAntwerpen
Faculty/Department
Research group
Project info
Dipeptidyl peptidases beyond glucose homeostasis: from biochemistry to physiological importance.
Publication type
Subject
Affiliation
Publications with a UAntwerp address
External links
Web of Science
Record
Identifier
Creation 13.04.2011
Last edited 15.11.2022
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