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 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.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Király K,Lambeir AM,Szalai J,Szentirmay A,Luyten W,Barna I,Puskár Z,Kozsurek M,Rónai AZdoi
10.1016/j.ejphar.2010.09.060subject
Has Abstractpub_date
2011-01-10 00:00:00pages
195-9issue
1eissn
0014-2999issn
1879-0712pii
S0014-2999(10)00981-7journal_volume
650pub_type
杂志文章abstract：:The cellular localisation and distribution of mRNAs encoding beta-adrenoceptor subtypes in human lung were studied by in situ hybridisation and Northern blot analysis. The 851-bp SmaI/PvuII fragment of human beta 1-adrenoceptor cDNA, the 439-bp SmaI fragment of human beta 2-adrenoceptor cDNA and the 975-bp SmaI fragme...
journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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abstract：:Rolipram was characterized for its emetic, behavioral, cardiovascular and pulmonary activities in dogs, to assess its systemic pharmacology and potential bronchodilatory selectivity. At doses > or = 0.1 mg/kg i.v., rolipram induced emesis, anxiety, and stepping behaviors in conscious dogs, and increased heart rate and...
journal_title：European journal of pharmacology
pub_type： 杂志文章
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