У роботі представлено результати дослідження аналгетичної та антиексудативної активності 2-(діетиламіно)етил-4-
[(11-оксоіндено[2,1-b]хіноксалін-6-карбоніл)аміно]бензоату на моделях термічного, хімічного болю й ексудативного запалення.
Досліджено мазі з різними концентраціями діючої речовини (1%, 3% і 5%). Найбільш виражену аналгетичну дію показала 5%-ва
мазь, яка сприяла зниженню больової реакції на 63,8% (у тесті «Гаряча вода») і на 66,5% (у тесті АІТЦ) порівняно з контрольною
групою. Антиексудативний ефект із застосуванням 5%-ї мазі був слабко вираженим у випадку зимозанового запалення та не проявлявся за наявності трипсинового запалення. Результати досліджень показали, що отримана сполука є перспективною для створення
місцевого аналгетика з комбінованим механізмом дії.
In medical practice, pain syndrome and inflammation are common clinical manifestations that significantly reduce the quality of life of
patients. A promising direction of modern pharmacotherapy is the development and search for local dosage forms with analgesic and antiinflammatory effects.
The aim of this work was to study the analgesic and anti-inflammatory activity of a new compound – 2-(diethylamino)ethyl-4-
[(11-oxoindeno[2,1-b]quinoxaline-6-carbonyl)amino]benzoate in the composition of ointments of different concentrations.
The study was conducted on 50 rats and 60 mice, in accordance with the requirements of GLP and ethical standards. The study of analgesic
activity was carried out on models of thermal (“hot water”) and chemical (allyl isothiocyanate test) pain. The assessment of anti-inflammatory
activity was carried out on models of exudative inflammation induced by trypsin and zymosan.
Research results. According to the results of the study, in the “hot water” test, 5% ointment based on 2-(diethylamino)ethyl-4-
[(11-oxoindeno[2,1-b]quinoxaline-6-carbonyl)amino]benzoate provided a significant reduction in pain sensitivity by 63.8%, and in the allyl
isothiocyanate test — 88 to 66.5% compared to the control group, which indicates a pronounced analgesic activity of the studied compound.
In the model of inflammation induced by zymosan, a moderate anti-exudative effect was established, which was manifested by a decrease in
the inflammatory reaction by 27.4%, while in the trypsin model no significant effect was recorded.
Thus, it was established that the studied compound is characterized by pronounced local analgesic activity and limited anti-inflammatory
properties, which depend on the type of model. The obtained results indicate the feasibility of further preclinical studies of the drug as a
potential local analgesic with a combined mechanism of action.
