Analgesic activity of 3-mono-substituted derivatives of dihydrofuran-2-one in experimental rodent models of pain.

Journal Title: Pharmacological Reports - Year 2009, Vol 61, Issue 5

Abstract

Three derivatives of dihydrofuran-2-one (L-PP, L-PP1, and L-SAL) were administered by intraperitoneal injection and their analgesic activity was assayed in several models of pain. The activity of these derivatives were tested using a hot plate test, a writhing test, capsaicin- and glutamate-induced nociception, along with two models of local anesthesia, including a test for infiltration anesthesia in guinea pigs and the modified tail immersion test in mice. The results of these in vivo experiments show that these three derivatives of dihydrofuran-2-one possess analgesic activity in rodents. The ED(50) values of the tested compounds are lower or comparable to the ED(50) values of reference compounds (acetylsalicylic acid or morphine). For the most active derivative of dihydrofuran-2-one, L-PP1 (3-[4-(3-trifluoromethylphenyl)-piperazin-1-yl]-dihydrofuran-2-one dihydrochloride), the ED(50) value was: 1.34 mg/kg, 0.79 mg/kg, 2.01 mg/kg and 3.99 mg/kg in the hot plate, writhing, capsaicin- and glutamate-induced pain tests, respectively.

Authors and Affiliations

Kinga Sałat, Barbara Filipek, Krzysztof Wieckowski

Keywords

Related Articles

Mechlorethamine (NTG) effects on the erythrocytic and leukocytic blood parameters during experimentally induced pleuritis in rats.

Background: According to cytotoxic and mutagenic properties, nitrogranulogen (NTG) changes the character of inflammatory reactions. Our previous studies have shown that NTG can enhance immunological defense reactions, be...

Enhancement of the anti-immobility action of antidepressants by risperidone in the forced swimming test in mice.

The aim of the present study was to examine the effect of antidepressants (ADs) belonging to different pharmacological groups and risperidone (an atypical antipsychotic drug), given separately or jointly, on immobility t...

Activation of orexin/hypocretin type 1 receptors stimulates cAMP synthesis in primary cultures of rat astrocytes.

The effects of orexins, which are also named hypocretins, on cAMP formation were examined in primary cultures of rat astrocytes. Orexin A, an agonist of OX(1) and OX(2) receptors, stimulated cAMP production with an EC(50...

Analysis of the role of Nrf2 in the expression of liver proteins in mice using two-dimensional gel-based proteomics.

Background: The transcription factor Nrf2 regulates expression of multiple cellular defence proteins through the antioxidant response element (ARE). Nrf2-deficient mice (Nrf2(-/-)) are highly susceptible to xenobiotic-me...

Effects of three calcium channel antagonists (amlodipine, diltiazem and verapamil) on the protective action of lamotrigine in the mouse maximal electroshock-induced seizure model.

The aim of this study was to assess the effect of three calcium channel antagonists (amlodipine, diltiazem and verapamil) on the anticonvulsant action of lamotrigine (a second generation antiepileptic drug) against maxim...

Download PDF file
  • EP ID EP107735
  • DOI -
  • Views 108
  • Downloads 0

How To Cite

Kinga Sałat, Barbara Filipek, Krzysztof Wieckowski (2009). Analgesic activity of 3-mono-substituted derivatives of dihydrofuran-2-one in experimental rodent models of pain.. Pharmacological Reports, 61(5), 807-818. https://europub.co.uk/articles/-A-107735