Р. В. Луценко, Антонина Григорьевна Сидоренко, Наталія Власенко, О. А. Луценко
{"title":"ВСТАНОВЛЕННЯ СЕРЕДНЬОЇ ЕФЕКТИВНОЇ ДОЗИ 2-ГІДРОКСИ-N- НАФТАЛЕН-1-ІЛ-2-(2-OКСО-1,2-ДИГІДРО-ІНДОЛ-3-ІЛІДЕН)-АЦЕТАМІДУ НА МОДЕЛІ «ПОВЕДІНКА, ЩО КАРАЄТЬСЯ»","authors":"Р. В. Луценко, Антонина Григорьевна Сидоренко, Наталія Власенко, О. А. Луценко","doi":"10.31718/mep.2022.26.1-2.05","DOIUrl":null,"url":null,"abstract":"Derivatives of 2-oxoindoline demonstrate significant biological and pharmacological activity, including diuretic, anti-inflammatory, antitumor, antiviral, antibacterial, analgesic, sedative, anticonvulsant and other effects. The aim of this research is to establish the average effective dose of 2-hydroxy-n-naphthalene-1-yl-2-(2-oxo-1,2-dihydro-indol-3-ylidene)-acetamide (compound 18) as a potential anxiolytic, as well as its therapeutic index. Materials and methods of research. The experiments were performed on 36 albino adult male Wistar rats. The average effective dose (ED50) of compound 18 for anxiolytic activity was investigated in the «punishable behavior» test. Rats were divided into 6 groups of 6 animals each. The dose range for the intraperitoneal route of administration was (1, 3, 6; 12, 24, 48 mg/kg). Results and discussion. The «punishable behavior» model, Vogel variant, determined the average effective dose (ED50) and dose-response relationship for 2-hydroxy-n-naphthalene-1-yl-2-(2-oxo-1,2-dihydro-indol-3-ylidene)-acetamide (compound 18) with a single intraperitoneal injection. Analysis of the results shows that the maximum dose that did not cause the effect was 1.0 mg/kg, the minimum effective dose ED16 was 4.5 mg/kg, and the maximum effective dose ED100 was 48 mg/kg. Conclusion. Experimentally determined ED50 of compound 18 in rats when administered intraperitoneally in the «punishable behavior» test, variant Vogel, was 11.9±2.85 mg/kg. The ED50 confidence margins were (4.92÷18.9) mg/kg. According to the therapeutic index, substance 18 exceeds diazepam by 14.8 times.","PeriodicalId":32911,"journal":{"name":"Problemi ekologiyi ta meditsini","volume":" ","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2022-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Problemi ekologiyi ta meditsini","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.31718/mep.2022.26.1-2.05","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0

摘要

2-氧吲哚啉衍生物具有显著的生物学和药理活性,包括利尿、抗炎、抗肿瘤、抗病毒、抗菌、镇痛、镇静、抗惊厥等作用。本研究的目的是建立2-羟基-n-萘-1-基-2-(2-氧-1,2-二氢吲哚-3-酰基)-乙酰胺(化合物18)作为潜在抗焦虑药的平均有效剂量及其治疗指标。研究材料和方法。实验以36只成年白化雄性Wistar大鼠为实验对象。在“惩罚行为”试验中考察了化合物18抗焦虑活性的平均有效剂量(ED50)。将大鼠分为6组,每组6只。腹腔给药剂量范围为(1,3,6;12、24、48 mg/kg)。结果和讨论。“惩罚行为”模型,Vogel变体,确定了单次腹腔注射2-羟基-n-萘-1-基-2-(2-氧-1,2-二氢吲哚-3-酰基)-乙酰胺(化合物18)的平均有效剂量(ED50)和剂量-反应关系。结果分析表明,不产生效应的最大剂量为1.0 mg/kg,最小有效剂量ED16为4.5 mg/kg,最大有效剂量ED100为48 mg/kg。结论。经实验测定,化合物18在大鼠“惩罚行为”试验(变异Vogel)中腹腔注射时的ED50为11.9±2.85 mg/kg。ED50置信边际为(4.92÷18.9) mg/kg。根据治疗指数,物质18超过安定14.8倍。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
ВСТАНОВЛЕННЯ СЕРЕДНЬОЇ ЕФЕКТИВНОЇ ДОЗИ 2-ГІДРОКСИ-N- НАФТАЛЕН-1-ІЛ-2-(2-OКСО-1,2-ДИГІДРО-ІНДОЛ-3-ІЛІДЕН)-АЦЕТАМІДУ НА МОДЕЛІ «ПОВЕДІНКА, ЩО КАРАЄТЬСЯ»
Derivatives of 2-oxoindoline demonstrate significant biological and pharmacological activity, including diuretic, anti-inflammatory, antitumor, antiviral, antibacterial, analgesic, sedative, anticonvulsant and other effects. The aim of this research is to establish the average effective dose of 2-hydroxy-n-naphthalene-1-yl-2-(2-oxo-1,2-dihydro-indol-3-ylidene)-acetamide (compound 18) as a potential anxiolytic, as well as its therapeutic index. Materials and methods of research. The experiments were performed on 36 albino adult male Wistar rats. The average effective dose (ED50) of compound 18 for anxiolytic activity was investigated in the «punishable behavior» test. Rats were divided into 6 groups of 6 animals each. The dose range for the intraperitoneal route of administration was (1, 3, 6; 12, 24, 48 mg/kg). Results and discussion. The «punishable behavior» model, Vogel variant, determined the average effective dose (ED50) and dose-response relationship for 2-hydroxy-n-naphthalene-1-yl-2-(2-oxo-1,2-dihydro-indol-3-ylidene)-acetamide (compound 18) with a single intraperitoneal injection. Analysis of the results shows that the maximum dose that did not cause the effect was 1.0 mg/kg, the minimum effective dose ED16 was 4.5 mg/kg, and the maximum effective dose ED100 was 48 mg/kg. Conclusion. Experimentally determined ED50 of compound 18 in rats when administered intraperitoneally in the «punishable behavior» test, variant Vogel, was 11.9±2.85 mg/kg. The ED50 confidence margins were (4.92÷18.9) mg/kg. According to the therapeutic index, substance 18 exceeds diazepam by 14.8 times.
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
自引率
0.00%
发文量
17
审稿时长
4 weeks
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信