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Eur J Pharmacol. 2011 Jan 10;650(1):195-9. doi: 10.1016/j.ejphar.2010.09.060. Epub 2010 Oct 15.

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

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Department of Pharmacology and Pharmacotherapy, Semmelweis University, POB 370, H-1445, Budapest, Hungary.


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 3nmol/rat vildagliptin could be antagonized by subcutaneous naltrexone (0.5mg/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 (1mg/kg) is a potent antihyperalgesic also when given subcutaneously.

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