ASSESSMENT OF NEW NONNARCOTIC ISOQUINOLINE DERIVATIVE ANALGESIC, COMPOUND G-104, FOR PRESENCE OF CONCOMITANT AND UNWANTED EFFECTS TYPICAL FOR ANALGESICS

Abstract

Aim. The aim of the study was to assess the effect of a new nonnarcotic analgesic, compound G-104, on the motor activity, coordination of movements, muscular tonus and respiratory function of white rats, when introduced in a wide range of doses comparing to the registered analgesics. Materials and methods. The effect on mice tonus was evaluated using the horizontally tightened wire, coordination of movements was studied with the device Rotarod, graphic registration of respiratory movements - by means of the system PowerLab 4/35 and the computer program LabChart 8. The number of respiratory movements per minute was calculated, the cases of pathological respiratory forms were taken into account. The motor activity was studied using the device “Open field”. Results. A new native analgesic G-104 does not influence the muscular tonus of white rats in the dose of UN50 unlike Tramadol and Ketorolac causing irreversible hypotonus in 50-100 % of experimental animals. The compound G-104, as well as the comparison drugs Tramadol and Ketorolac, has no effect on coordination of movements. No changes in spontaneous motor activity after chronic introduction of G-104 in the device “Open field” were revealed. A new analgesic G-104 does not alter the frequency and amplitude of white rats’ respiratory movements when introduced in the dose of UN50 as compared with the background indices. Conclusions. The compound G-104, when introduced in the dose of UN50, does not influence the muscular tonus and coordination of movements in white rats unlike the analgesics Tramadol and Ketorolac causing hypotonus in therapeutic doses. The compound G-104 does not alter the spontaneous motor activity in the device “Open field”. A new analgesic G-104 does not depress respiration in white rats when introduced in the dose of UN50.

Keywords

Nonnarcotic analgesic G-104 / Ketorolac / Tramadol / white rats / spontaneous motor activity / muscular tonus / coordination of movements / respiratory function

References

[1] Буреш Я., Бурешова О., Хьюстон Дж.П. Материалы и основные эксперименты по изучению мозга и поведения. М.: Высшая школа 1991; 397.

[2] Вихарев Ю.Б. Противовоспалительная и анальгетическая активности производных 3,3-диалкил-3,4-дигидроизохинолинов и фенэтиламидов: автореф. дис. … канд. биол. наук. Томск 2005; 23.

[3] Зенкова Е.А., Вдовина Г.П., Данилова В.К., Бурлуцкая А.А., Чугунова М.П., Астафьева С.А., Шкляев Ю.В. Исследование анальгетической активности и оценка вовлеченности опиоидной системы в реализацию антиноцицептивного эффекта производного изохинолина и гексановой кислоты соединения Г-104 в сравнении с наркотическим анальгетиком. Proceedings of materials the international scientific conference «News of science». Czech Republic, Karlovy Vary - Russia, Moscow, 30-31 August 2015, available at: http://books.eee-science.ru/downloads/news-of-science/.

[4] Чурюканов В., Чурюканов М. Фармакология болеутоляющих средств. Врач 2002; 4: 29-33.

[5] Руководство по проведению доклинических исследований лекарственных средств. Ч. I. Под ред. А.Н. Миронова. М.: Гриф и К 2012; 944.

RIGHTS & PERMISSIONS

Zenkova E.A., Vdovina G.P., Burlutskaya A.A., Danilova V.K.