Study of Anti-inflammatory Activity of a New Non-opioid Analgesic on the Basis of a Selective Inhibitor of TRPA1 Ion Channels
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Published:2019-07-24
Issue:2
Volume:18
Page:110-125
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ISSN:1871-5230
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Container-title:Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
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language:en
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Short-container-title:AIAAMC
Author:
Beskhmelnitsyna Evgeniya A.1, Pokrovskii Mikhail V.1, Kulikov Aleksandr L.2, Peresypkina Anna A.1, Varavin Evgeniy I.3
Affiliation:
1. Department of Pharmacology and Clinical pharmacology, Medical Faculty of Belgorod National Research University, 85 Pobeda St., Belgorod, 308015, Russian Federation 2. Research Institute of Pharmacology of Living systems of Belgorod National Research University, 85 Pobeda St., Belgorod, 308015, Russian Federation 3. Physician Training Faculty for Aerospace Forces of Kirov Military Medical Academy, 6 Academician Lebedev St., Saint Petersburg, 194044, Russian Federation
Abstract
Introduction:
Nowadays, the group of NSAIDs is used the most widely in order
to treat the inflammatory process. But its long-term administration increases the risk of
complications of pharmacotherapy. Therefore, today it is urgent to search for new molecules
that can selectively block biological targets that directly perceive inflammatory mediators.
One of such targets is TRPA1. ZC02-0012, a compound from the group of substituted
pyrazinopyrimidinones, which is a selective inhibitor of TRPA1 ion channel.
Objective:
The aim of our study was to study the anti-inflammatory activity of an innovative
molecule under the laboratory code ZC02-0012 from the group of selective inhibitors
of TRPA1 ion channel.
Materials and Methods:
Anti-inflammatory activity of ZC02-0012 was studied on the
model of acute exudative inflammation of the paw in response to subplantar injection in
the right hind paw of mice with 0.02 ml of 2% formaldehyde solution. The mass of the
paw was measured after 4 hours (peak edema) after phlogistic injection. The test substance
and the reference drug was administered intragastrically or intramuscularly 45 minutes before
the injection of formaldehyde solution. The presence and intensity of antiinflammatory
activity was judged by the inhibitory effect, represented in percent.
Results and Discussion:
Selective inhibitor of the TRPA1 ion channel ZC02-0012 revealed
the anti-inflammatory activity at doses of 3 and 9 mg/kg, its intensity is comparable to diclofenac
sodium.
Conclusion:
The selective inhibitor of the ion channel TRPA1, a substance under code
ZC02-0012, has an anti-inflammatory activity comparable with diclofenac sodium.
Publisher
Bentham Science Publishers Ltd.
Subject
Pharmacology,General Medicine,Immunology,Immunology and Allergy
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