> Cipher: ВУ45/2020/41 Journal 2020year № 41 Volotovska, N. V. Study of morphological changes in the kidney during modeling of ischemic-reperfusion injuries of the limb and massive blood loss / N. V. Volotovska. - С.5-10. - Bibliogr. at the end of the art. Ivankova, A. V. Comparative assessment of renal function by cystatin С level in patients with hypertension and extrasystole / A. V. Ivankova [та ін.]. - С.11-17. - Bibliogr. at the end of the art. Other authors: Kuzminova N. V., Lozinsky S. E., Ivanov V. P. Drachevska, I. Yu. Determination of cephalometnc parameters which usually do not change during surgical and orthodontic treatment depending on facial types according to Garson in Ukrainian young men and young women with orthognathic occlusion / I. Yu. Drachevska [та ін.]. - С.18-23. - Bibliogr. at the end of the art. Other authors: Dmitriev М. O., Perera Clifford, Shevchenko V. М., Gunas I. V. Grebeniuk, D. I. Evaluation of the effect of excess and deficiency of serum hydrogen sulfide on the condition of the vaginal wall of intact rats / D. I. Grebeniuk [та ін.]. - С.24-29. - Bibliogr. at the end of the art. Other authors: Voloshchuk N. I., Taran I. V., Gormash P. P., Nazarchuk O. A. Halushka, A. М. Actual aspects of traumatic pathology among servicemen of Ukrainian Armed Forces in Joint Forces Operation / A. М. Halushka [та ін.]. - С.30-35. - Bibliogr. at the end of the art. Other authors: Khalik S. V., Rychka О. V., Lopin Ye. B. Malchenko, О. V. Investigation of 4-methyl-2 2-dioxo-1h-2Ae.1-benzothiazine- 3-carboxamide derivative influence on the biochemical markers of gastric mucosa in rats / О. V. Malchenko, N. I. Voloschuk, N. O. Pentiuk. - С.36-40. - Bibliogr. at the end of the art. Samborska, I. A. Changes in the histostructure of the lungs of old rats under conditions of persistent hyperhomocysteinemia / I. A. Samborska. - С.41-45. - Bibliogr. at the end of the art. Bondarenko, P. S. Investigation of pharmacokinetics of N-(4-trifluoromethylphenyl)-4-methyl-2.2-dioxo-1H-2λ6.1-benzothiazine-3-carboxamide various crystalline modifications in vivo / P. S. Bondarenko [та ін.]. - С.46-51. - Bibliogr. at the end of the art. Other authors: Voloshchuk N. I., Larionov V. B., Fedoseenko Η. O. Vakhovskyi, V. V. Correlations of basal cranial structures characteristics determined by Bjork and Jarabak methods with teleradiographic parameters of the upper and lower jaws and tooth location in young men and young women with orthognathic occlusion / V. V. Vakhovskyi [та ін.]. - С.52-59. - Bibliogr. at the end of the art. Other authors: Shinkaruk-Dykovytska М. М., Pogorila A. V., Likhitskyi O. O., Gunas I. V. Khasawneh, Ahmad Raed. Correlations between the severity of oily skin and the emotional impact of oily skin with anthropo-somatotypological parameters of men and women with seborrheic dermatitis / Ahmad Raed Khasawneh [та ін.]. - С.60-66. - Bibliogr. at the end of the art. Other authors: Dmytrenko S. V., Kizina I. E., Kyrychenko Yu. V., Prokopenko S. V. The copies are in the departments: total 1 Free: 1 |
Malchenko, О. V. Investigation of 4-methyl-2 2-dioxo-1h-2Ae.1-benzothiazine- 3-carboxamide derivative influence on the biochemical markers of gastric mucosa in rats [Text] / О. V. Malchenko, N. I. Voloschuk, N. O. Pentiuk> // Biomedical and Biosocial Anthropology. - 2020. - № 41. - С. 36-40. - Bibliogr. at the end of the art. MeSH-main: БОЛЕЗНЬ, МОДЕЛИ НА ЖИВОТНЫХ -- DISEASE MODELS, ANIMAL ПРОТИВОВОСПАЛИТЕЛЬНЫЕ СРЕДСТВА НЕСТЕРОИДНЫЕ -- ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL (анализ, токсичность) ПРОЛЕКАРСТВА -- PRODRUGS (анализ, терапевтическое применение, фармакология) ПОБОЧНЫЕ ЭФФЕКТЫ И НЕБЛАГОПРИЯТНЫЕ РЕАКЦИИ, СВЯЗАННЫЕ С ЛЕКАРСТВАМИ -- DRUG-RELATED SIDE EFFECTS AND ADVERSE REACTIONS (этиология) ЛЕКАРСТВ ОЦЕНКА ДОКЛИНИЧЕСКАЯ -- DRUG EVALUATION, PRECLINICAL (методы, тенденции) ЖЕЛУДКА СЛИЗИСТАЯ -- GASTRIC MUCOSA (действие лекарственных препаратов) ТАБЛИЦЫ -- TABLES Annotation: Non-steroidal anti-inflammatory drugs occupy a leading position in the pharmaceutical market, but their class-specific side effect (ulcerogenic action) significantly limits their widespread use. The N-(4-methoxybenzyl)-4-methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamide derivative (compound NI-9) showed a pronounced analgesic effect in various models of pain syndromes. The aim of the study was to determine the effect of a new original derivative of 4-methyl-2.2-dixo-1H-2λ6,1-benzothiazine-3-carboxylic acid on the macroscopic state and biochemical parameters of the gastric mucosa of rats. The study was performed on 51 male Wistar rats. Compound NI-9 and the reference drug meloxicam were administered intragastrically once daily for 28 days at doses of 3 and 5 mg/kg, corresponding to their ED50 analgesic activity. Macroscopic indicators of GM damage, glycosaminoglycan content, phospholipid profile, level of MDA and CGP, as well as nitrates and nitrites and H2S were determined. The results were processed in the program STATISTICA 10.0 using non-parametric methods. The results showed that the carboxamide derivative was safer for the stomach because the ulcer index of compound NI-9 was 1.73 times lower than that of meloxicam. The damaging effect of the compound was more pronounced at the pre-epithelial and epithelial levels of GM protection, while the post-epithelial level (production of vasodilating molecules NO and H2S) was practically unaffected by this derivative, unlike meloxicam, which caused damage at all levels of protection. The obtained data supplement the data on the pharmacodynamics of the 4-methyl-2.2-dixo-1H-2λ6,1-benzothiazine-3-carboxylic acid derivative and determine the expediency of its further studies as a potential non-opioid analgesic Additional Access Points: Voloshchuk, N. I. Pentiuk, N. O. There are no free copies |
> Cipher: ВУ45/2021/42 Journal 2021year № 42 Oshurko, A. P. Morphological features of bone tissue in "disuse atrophy" on the example of a segment of the human lower jaw: clinical experience of treatment / A. P. Oshurko [та ін.]. - С.5-11. - Bibliogr. at the end of the art. Other authors: Oliinyk I. Yu., Yaremchuk N. I., Makarchuk I. S. Kulbitska, V. V. Histological changes of the adrenal glands vessels after experimental thermal trauma and under the conditions of lyophilized xenoskin use / V. V. Kulbitska. - С.12-17. - Bibliogr. at the end of the art. Malakhov, V. O. Safety of transcranial magnetic stimulation in patients with multiple sclerosis / V. O. Malakhov, P. K. Gaponov. - С.18-22. - Bibliogr. at the end of the art. Zykova, N. P. Microscopic changes of the pancreas vessels in the dynamics after experimental thermal injury / N. P. Zykova. - С.23-28. - Bibliogr. at the end of the art. Fedosieieva, О. V. The effect of prenatal action of dexamethasone on morphological changes of the thyroid gland stromal compartment in juvenile rats / О. V. Fedosieieva, V. S. Bushman. - С.29-33. - Bibliogr. at the end of the art. Ohinska, N. V. Reorganization of cerebellar cortex structural components one day after experimental thermal injury / N. V. Ohinska. - С.34-38. - Bibliogr. at the end of the art. Mostovoy, Y. M. Features of the COPD course in patients with different alleles of C79G (rs1072714) of ADRB2 gene / Y. М. Mostovoy, K. D. Dmytriiev, N. S. Slepchenko. - С.39-43. - Bibliogr. at the end of the art. Osovska, N. Y. Associations of excess myocardial mass, echoreflectiveness and aldosterone synthase gene polymorphism in men with hypertension / N. Y. Osovska [та ін.]. - С.44-51. - Bibliogr. at the end of the art. Other authors: Lozinska M. S., Lozinsky S. E., Taran I. V., Mazur Y. V., Dovganiuk I. E., Gribenuk О. V., Kuzminova N. V. Bahrij, D. A. Clinical significance of single nucleotide missense-mutation rs950880 of the IL1RL1 gene in patients with essential hypertension / D. A. Bahrij. - С.52-46. - Bibliogr. at the end of the art. Malchenko, О. V. In-depth investigation of analgesic activity of N-(4-methoxybenzyl)-4-methyl-2.2-dioxo-1H-2 λ6.1-benzothiazine-3-carboxamide derivate on different models of pain perception / О. V. Malchenko. - С.57-63. - Bibliogr. at the end of the art. The copies are in the departments: total 1 Free: 1 |
Malchenko, О. V. In-depth investigation of analgesic activity of N-(4-methoxybenzyl)-4-methyl-2.2-dioxo-1H-2 λ6.1-benzothiazine-3-carboxamide derivate on different models of pain perception [Text] / О. V. Malchenko> // Biomedical and Biosocial Anthropology. - 2021. - № 42. - С. 57-63. - Bibliogr. at the end of the art. Rubrics: Диклофенак--животное--тер прим Мелоксикам (Мовалис)--тер прим--фарм MeSH-main: БОЛЕЗНЬ, МОДЕЛИ НА ЖИВОТНЫХ -- DISEASE MODELS, ANIMAL ДИАБЕТИЧЕСКИЕ НЕВРОПАТИИ -- DIABETIC NEUROPATHIES (патофизиология, этиология) АРТРИТ ЭКСПЕРИМЕНТАЛЬНЫЙ -- ARTHRITIS, EXPERIMENTAL (патофизиология, этиология) БЕНЗОАТЫ -- BENZOATES (анализ) КАРБОНОВЫЕ КИСЛОТЫ -- CARBOXYLIC ACIDS (анализ) ДИАГРАММЫ -- CHARTS ТАБЛИЦЫ -- TABLES Annotation: Among N-(4-methoxybenzyl)-4-methyl-2.2-dioxo-1H-2 λ6.1-benzothiazine-3-carboxamide derivates, the compound methoxybenzyl-amide derivative 4-methyl-2.2-dioxo-1H-2λ6.1-benzothiazine-3-carboxylic acid (compound NI-9) with pronounced analgesic and anti-inflammatory activities, which was superior to those of diclofenac and lornoxicam in the model of carrageenan edema. The aim of the study was to investigate the analgesic effect of benzothiazine-3-carboxamide derivative on different models of somatic and neuropathic pain syndromes. The study was performed on 91 male Wistar rats. Compound NI-9 and reference drugs meloxicam, diclofenac and gabapentin were administered intragastrically at doses of 3, 5, 8 and 5 mg/kg, respectively, corresponding to their ED50 in analgesic activity. Acetic spasms in mice, a model of thermal irritation of the tail flick in rats, as well as adjuvant arthritis and diabetic polyneuropathy were selected as models of pain syndromes. The results were processed in the program STATISTICA 10.0 using non-parametric methods. The results showed that methoxybenzyl-amide derivative 4-methyl-2.2-dioxo-1H-2λ6.1-benzothiazine-3-carboxylic acid (compound NI-9) has a pronounced analgesic effect on various models of pain syndromes, both somatic and inflammatory. and of neurogenic origin. The analgesic activity of the compound NI-9 in the model of acetic acid cramps in mice and thermal irritation in rats was 38.09 and 49.75 %, respectively, which was higher than that of meloxicam (36.73 and 45.68 %), and inferior to diclofenac (41.95 and 55.95 %). In the model of the systemic inflammatory process (adjuvant arthritis), the analgesic effect of NI-9 was statistically superior to meloxicam and diclofenac (43.32 % vs. 26.26 and 33.69 %). In a model of neuropathic pain syndrome (diabetic neuropathy), the analgesic effect of methoxybenzyl-amide derivative 4-methyl-2.2-dioxo-1H-2λ6.1-benzothiazine-3-carboxylic acid was greater than meloxicam (18.96 vs. 13.34 %), but this figure was lower than that of gaapentin (20.83 %). Further in-depth study of its pharmacodynamics and toxicity will be the theoretical basis for the development on the basis of this biologically active compound of the original drug with analgesic and anti-inflammatory activities There are no free copies |