DOI: https://doi.org/10.22263/2312-4156.2023.5.67
A.A. Vasilyuk
Anti-inflammatory activity of a number of new piperidine derivatives with substitutions in the 1st and the 4th positions
Grodno State Medical University, Grodno, Republic of Belarus
Vestnik VGMU. 2023;22(5):67-72.
Abstract.
Objectives. To study the anti-inflammatory activity of 13 new piperidine derivatives with substitutions in the 1st and the 4th positions.
Material and methods. For studying the anti-inflammatory activity, a model of acute exudative inflammation was used; lambda-carrageenan acted as a phlogogen. Rats were subcutaneously injected the test compounds/comparison analgesic diclofenac sodium, followed by intraplantar injection of carrageenan 30 minutes later. Oncometrically we assessed the initial volume of the limb (before the introduction of phlogogen) and the volume of the limb in 1.5 hours, 3 hours and one day after the start of the experiment.
Results. 4 out of 7 studied piperidine derivatives demonstrated anti-inflammatory activity in one or more doses – AGV-22, 23, 24, 31. At the same time, a high anti-inflammatory potential can be noted in the compound AGV-22, the activity of which at a dose of 20 mg/kg in this series of experiments is comparable to the activity of the reference drug diclofenac. AGV-22 statistically significantly reduced the exudative process in the late phase of exudation (24 hours after administration of carrageenan) at a dose of 10 mg/kg and in all phases of carrageenan edema at a dose of 20 mg/kg. The anti-inflammatory activity of other compounds was an order of magnitude lower: AGV-24, AGV-31 and AGV-23 reduced paw swelling only at certain stages of edema.
Conclusions. A new piperidine derivative with substitutions in the 1st and the 4th positions, AGV-22, combines high analgesic and anti-inflammatory activity. The anti-inflammatory effect of AGV-22 may be due to inhibition of cyclooxygenase and suppression of the inflammatory prostaglandins synthesis, and the spectrum of pharmacological activity is similar to non-steroidal anti-inflammatory drugs.
Keywords: inflammation, pain, anti-inflammatory activity, carrageenan edema, piperidine derivatives, non-steroidal anti-inflammatory drugs.
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Information about authors:
A.A. Vasilyuk – postgraduate of the Chair of Pharmacology named after Professor M.V. Korablev, Grodno State Medical University,
e-mail: Этот адрес электронной почты защищён от спам-ботов. У вас должен быть включен JavaScript для просмотра. – Anna A. Vasilyuk.
