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Title
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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
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Author
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Abstract
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| 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. |
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Language
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English
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Source (journal)
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European journal of pharmacology. - Amsterdam, 1967, currens
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Publication
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Amsterdam
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North-Holland
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2011
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ISSN
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0014-2999
[print]
1879-0712
[online]
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DOI
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10.1016/J.EJPHAR.2010.09.060
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Volume/pages
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650
:1
(2011)
, p. 195-199
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ISI
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000285893800026
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Full text (Publisher's DOI)
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