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2019 CSHP National Awards Program Winners
- , 2019,
Abstract: Sponsored by Teva Canada Limite
镇静催眠天然植物有效成分研究进展
Advances in Sedative-Hypnotic Natural Plant Active Ingredients
 [PDF]

张莹, 马密霞, 王刚, 付梦蕾, 曲有乐, 胡文祥
Journal of Comparative Chemistry (CC) , 2018, DOI: 10.12677/CC.2018.22009
Abstract:
本文叙述了具有镇静催眠作用的植物有效部位及植物活性成分,这些植物中不同种类的化学成分均具有不同程度的镇静催眠作用,有明确的分子结构的化学成分的集结,将为镇静催眠药物的合成及结构改造提供直观的物质基础。
By retrieving relevant literature, experimental research progress was given, as so as the sedative and hypnotic effects of plant effective part and the active ingredient. Different types of chemical composition of these plants have sedative and hypnotic effects in varying degrees. It is clear that their chemical composition of molecular structure will provide the intuitive material basis for the sedative hypnotic drugs synthesis and structural modification. They play the role not only to provide the material basis for plants sedative-hypnotic effects, but also to find and develop new sedative hypnotic drugs experimental basis.
Evaluation of phytochemical constituents and sedative-hypnotic activity of the methanol leaf extract of Ficus exasperata in mice
Aishatu Ummi Zaifada,David Dezi Akumka,Hudu Garba Mikail,Mohammed Adamu
- , 2019, DOI: 10.14202/vetworld.2019.830-833
Abstract:
调中化痰安神合剂镇静催眠作用的药效学研究
徐琦,蔡铁如
中国中医药信息杂志 , 2015,
Abstract: 目的 探讨调中化痰安神合剂镇静催眠的作用机制。方法 健康昆明种小鼠200只,随机分为4组各50只,各组又随机分为空白组、对照组和调中化痰安神合剂高、中、低剂量组(中药高、中、低剂量组),每组10只,分别予生理盐水、艾司唑仑和高、中、低剂量调中化痰安神合剂灌胃给药,每日1次。第1组连续给药7 d,观察各组小鼠给药前后自发活动的次数。第2组连续给药7 d,给药结束60 min后,各组小鼠予戊巴比妥钠30 mg/kg体质量(引起100%小鼠睡眠的最小阈剂量)腹腔注射,记录各组小鼠的睡眠时间。第3组连续给药7 d,给药结束60 min 后,各组小鼠予戊巴比妥钠15 mg/kg体质量(引起90%~100%小鼠翻正反射不消失的最大剂量)腹腔注射,观察并记录入睡动物数,计算入睡率。第4组连续给药15 d后脱颈处死,迅速取出脑组织,分批取出匀浆,荧光分光光度法测定小鼠脑组织中5-羟色胺(5-HT)、5-羟吲哚乙酸(5-HIAA)含量。结果 与空白组比较,各给药组小鼠活动次数减少、睡眠潜伏期缩短、睡眠持续时间延长、入睡率提高(P<0.01,P<0.05),其中对照组和中药高剂量组镇静效果明显优于其他给药组,差异有统计学意义(P<0.05),但2组比较差异未见统计学意义(P>0.05)。与空白组比较,各给药组小鼠脑内5-HT、5-HIAA含量增加,差异有统计学意义(P<0.01,P<0.05),中药高剂量组增加最显著(P<0.05)。结论 调中化痰安神合剂有明显镇静催眠作用,其作用机制可能与增加脑内5-HT合成与代谢有关
小新塔花水提物对小鼠镇静催眠及免疫功能的影响
沙爱龙
- , 2016, DOI: 10.13982/j.mfst.1673-9078.2016.5.04
Abstract: 本文研究了小新塔花水提物对小鼠镇静催眠及免疫功能的影响。实验用不同剂量的小新塔花水提物作用于小鼠,观察记录小鼠自发活动次数,采用阈剂量戊巴比妥钠睡眠实验法和阈下剂量戊巴比妥钠诱导小鼠睡眠实验,观察小新塔花水提物镇静催眠作用。用分光光度法、酶联免疫法、称重法及观察法研究小新塔花水提物对小鼠免疫功能的影响和急性毒性试验。结果表明,与正常对照组相比,小新塔花水提物中、高剂量组对小鼠走动次数、举双前肢数、入睡数和睡眠时间的影响差异显著(p<0.05)或极显著(p<0.01),且呈剂量依赖效应;小新塔花水提物3个剂量组的小鼠胸腺指数、脾脏指数、血清酸性磷酸酶(ACP)、溶菌酶(LYZ)活性及免疫球蛋白(IgG)含量均有所增加,且大都差异显著(p<0.05)或极显著(p<0.01);小新塔花水提物毒性小,安全范围大。结果提示,小新塔花水提物具有明显的镇静催眠、增强免疫功能作用。
The impact of sedative-hypnotic effects of aqueous extract of Ziziphora tenuior Linn. on the immune function in mice was investigated in this study. The effects of the aqueous extract of Z. tenuior on spontaneous activity, dormancy-number, and dormancy-time of mice induced by pentobarbital sodium were observed and compared with that in the physiological saline-treated groups. Further, the thymus index, spleen index, activities of ACP and LYZ, and the concentration of IgG in the sera of mice treated with three doses of the aqueous extract of Z. tenuior were determined. For acute toxicity tests, the aqueous extracts were orally administered. The results showed that in the medium- and high-dose groups for the aqueous extract of Z. tenuior, spontaneous activity was significantly inhibited, and both dormancy-number and -time were significantly increased in the mice induced by pentobarbital sodium, when compared with those in the physiological saline-treated groups. Moreover, these effects were dose-dependent. The three doses of the aqueous extract of Z. tenuior also significantly increased the thymus index, spleen index, activities of ACP and LYZ, and the concentration of IgG in the mice sera. The aqueous extract of Z. tenuior was nontoxic, and showed a large safety range. The results indicated that the aqueous extract of Z. tenuior had obvious sedative and hypnotic effects in mice, and there was a synergistic effect between the extracts and pentobarbital sodium, which could significantly strengthen immune function in mice.
Hydroalcoholic Tarooneh Extract (Spathe of Phoenix Dactylifera) Increased Sedative-hypnotic Effects and Modulated Electroencephalography Brain Waves in Anesthetized Rats
Ali Asghar Pourshanazari,Bahare Zarrin,Hojjatollah Alaei,Parham Reisi,Sahar Rahimi,Zahra Siahmard
- , 2019, DOI: 10.4103/abr.abr_58_16
Abstract: Spathe of phoenix dactylifera is hard-covering envelope of date palm which is mentioned as a nerve relief in ancient medicine books. In this experiment, three extract doses used in sleeping time, sedative efficacy, and electroencephalography (EEG) protocol to show different aspects of extract effects on sleep
The central nervous system depressant activities of Mycotoxin MT81 and its Acetylated and Benzoylated analogues
Sujata Maiti Choudhury
Al Ameen Journal of Medical Sciences , 2008,
Abstract: Mycotoxin MT81 isolated from Penicillium nigricans and its two structural derivatives viz. Acetylated MT81 (AcMT81) and Benzoylated MT81 (BzMT81) show antimicrobial activities as well as cause hepatotoxicity and nephrotoxicity. Present study deals with the CNS depressant activity of the above said toxins. Sedative-hypnotic and hypothermic actions were assessed by injecting MT81, AcMT81, and BzMT81 at three different doses prior to the administration of diazepam, chloropromazine and pentobarbitone respectively. The analgesic actions were studied by hot plate method. The sleep induced by diazepam, chlorpromazine and pentobarbitone were prolonged following the administration of MT81, AcMT81 and BzMT81. Significant hypothermia produced in a dose-dependent manner after the treatment with MT81 and its two derivatives. The toxins also potentiated the analgesic action of morphine significantly (p≤0.001). Being less toxic than the parent toxin MT81, the structural analogues showed more prominent analgesic activities, sedative effects and hypothermic actions.
Studies of CNS Activities of Some Mannich bases of 1,3,4-Oxadiazole
R.R. Somani,G. Kadam,R. Vohra,S. Vijayaraghavan
International Journal of Pharmacology , 2010,
Abstract: The present study demonstrated the various Central Nervous System effects like depressant, sedative-hypnotic, anticonvulsant and anxiolytic activities of some Mannich bases of 2,5-disubstituted-1,3,4-oxadiazole on albino mice. Before their evaluation for Central Nervous System activities, these derivatives were subjected to preliminary screening for anticonvulsant activity and toxicity studies concluding that the compounds are non toxic and Central Nervous System depressant in nature. Various animal models were utilized, such as, for depressant activity: ambulatory activity, Hole-board and Rotarod; for sedative-hypnotic activity: Ketamine-induced sleeping time; for anticonvulsant activity: Maximum Electroshock, Pentylene tetrazole induced convulsions and Strychnine induced convulsions; for anxiolytic activity: Staircase test, Elevated Plus Maze model. It was found that the test compounds of doses 50, 100 and 150 mg kg-1, showed significant dose dependent increase in the above Central Nervous System activities when administered intra peritoneally.
EcoDopplercardiografia em coelhos: uso de midazolam e midazolam associado à cetamina
Silva, E.F.;Borboleta, L.R.;Telles, T.C.;Fonseca, V.B.;Melo, M.M.;
Arquivo Brasileiro de Medicina Veterinária e Zootecnia , 2011, DOI: 10.1590/S0102-09352011000600017
Abstract: the use of animals as experimental models often requires anesthesia, particularly when it comes to echocardiographic evaluation of rabbits. however, there is little information regarding the protocols and their effects on echocardiographic parameters. we used 20 male five month old new zealand rabbits, weighing 3.2kg, distributed in two groups of 10 animals each: g1 - midazolam maleate associated with ketamine hydrochloride, and g2 - midazolam maleate. we compared the effect of two protocols on functional indicators of the left ventricle and the flow valves and we obtained lower values of heart rate and left ventricular ejection fraction and higher values of left ventricular diameter in systole, end-systolic volume of left ventricle and aortic diameter in the group that received only midazolam. midazolam maleate was more effective because it promoted good sedation, allowing a good quality examination and limited effects on the cardiovascular system.
Psychopharmacological Profile of Hydroalcoholic Extract and P-Hydroxybenzoic Acid Obtained from Bourreria huanita (Boraginaceae) in Mice  [PDF]
Iandra Holzmann, Daiane Cattani, Micheli Corso, Daiane Perondi, Sabrina Zanella, Cristiani Burger, Luiz Carlos Klein Júnior, Valdir Cechinel Filho, Sully M. Cruz, Miguel F. Torres, Armando Cáceres, Márcia Maria de Souza
Pharmacology & Pharmacy (PP) , 2014, DOI: 10.4236/pp.2014.511110
Abstract: Bourreria huanita (Lex.) Hemsl. (Boraginaceae) is a very rare and highly appreciated tree in Mesoamerica for its medicinal properties and beauty. It grows in a region extending from central Mexico to Costa Rica. Ethnobotanical surveys have shown that the infusion of dried flowers is popularly used as a tranquilizer to cure several diseases. In the present study we report the isolation of p-hydroxybenzoic acid (pHBZ) obtained from the hydroalcoholic extract (HE) of B. huanita, and the effect of both, the extract and the compound on the central nervous system in mice. HE of B. huanita (100, 150, 300 mg/kg) and pHBZ (10 mg/kg) were orally administered to mice and 1 h later, behavioral tests were performed. The effects of HE and pHBZ were tested by pentylenetetrazole (PTZ) and strychnine (STR) induced seizures, pentobarbital-induced hypnosis, the forced swimming test and the tail suspension test, the elevated plus maze, apomorphine-induced stereotypy and the climbing test, the inhibitory avoidance test and the open-field test. B. huanita extract produced hypnotic, anxiolytic and antidepressant effects in animals, with no change in motor performance. On the other hand, the extract did not reduce PTZ and STR-induced convulsions, apomorphine-induced stereotypy or climbing. Moreover, no changes were observed in the animals’ memory. The compound pHBZ was effective only in the depression tests. The results obtained in the present study suggest that B. huanita exhibited sedative, antidepressant and hypnotic activities in mice, and that the antidepressant activity may be mediated by an isolated compound identified as pHBZ.
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