Sedative–hypnotic effect of YZG-330 and its effect on chloride influx in mouse brain cortical cells

This study was to examine the sedative–hypnotic effect of YZG-330 and its influence on Cl−influx in mouse cortical cells.In a sleep time-prolongation test in which mice were administered a threshold dosage of sodium pentobarbital(ip),YZG-330(0.125,0.5 and 2 mg/kg,po)prolonged the sleep time by 25%(P40.05),64%(Po0.01)and 506%(Po0.001),respectively.Thereafter,treatment with YZG-330 permitted mice that had woken up after the threshold dose of sodium pentobarbital(ip)to fall asleep again.A Cl−-sensitive fluorescent probe,N-(ethoxycarbonylmethyl)-methoxyquinolinium bromide(MQAE),was used to determine the effect of YZG-330 on Cl−influx.YZG-330(0.3,0.6 and 1.5 mM)increased Cl−influx in mouse cortical cells in a concentration-dependent manner.These data suggest that YZG-330 has a hypnotic effect in mice,and the effect may be related to an increase in Cl−influx in cortical cells.

Sedative and Hypnotic Effects and Transcriptome Analysis of Polygala tenuifolia in Aged Insomnia Rats

Objective:To study the sedative and hypnotic effects and underlying mechanisms of Polygala tenuifolia(PT)on treating aged insomnia rats.Methods:Sixty Sprague-Dawley male rats were divided into 6 groups by a random number table,including control group,model group,diazepam group(0.92 mg/kg),as well as PT low-,medium-and high-dose groups(0.0875,0.175,0.35 g/kg,respectively),10 rats in each group.Aged insomnia rat model was established with subcutaneous injection of D-galactose for 42 days and then intraperitoneal injection of para-chlorophenylalanine for 3 days.PT and diazepam were respectively given to aged insomnia rats by intragastric administration for 7 days after model establishment.Then the rats were investigated by body weight,Morris water maze test,pentobarbital test,enzyme-linked immunosorbent assay,and transcriptome sequencing.Results:Compared with the model group,PT increased the body weight,improved memory ability,and prolonged pentobarbital-induced sleep time of aged insomnia rats(P<0.01 or P<0.05).The medium dose of PT also increased the neurotransmitter levels of 5-hydroxytryptamine(5-HT)and gamma-aminobutyric acid(GABA),and decreased the level of Glu in the hippocampus of aged insomnia rats(P<0.05 or P<0.01).Twenty-four differentially expressed genes(DEGs)were overlapped among model group,medium-dose PT group,and diazepam group in transcriptome analysis.Fuom and Pcp2 were down-regulated by the treatment of medium-dose PT(P<0.01 or P<0.05).The metabolic pathways of PT were relatively less than diazepam(91 vs.104).Conclusions:The sedative and hypnotic effects of PT in aged insomnia rats might be related to neuro,metabolism pathways,especially through GABAergic signaling pathway.It provided more effective herb choice for the treatment of senile insomnia.

Sedation in gastrointestinal endoscopy: Where are we at in 2014?

Gastrointestinal endoscopies are invasive and unpleasant procedures that are increasingly being used worldwide. The importance of high quality procedures(especially in colorectal cancer screening), the increasing patient awareness and the expectation of painless examination, increase the need for procedural sedation. The best single sedation agent for endoscopy is propofol which, due to its' pharmacokinetic/dynamic profile allows for a higher patient satisfaction and procedural quality and lower induction and recovery times, while ma-intaining the safety of traditional sedation. Propofol is an anesthetic agent when used in higher doses than those needed for endoscopy. Because of this important feature it may lead to cardiovascular and respiratory depression and, ultimately, to cardiac arrest and death. Fueled by this argument, concern over the safety of its administration by personnel without general anesthesia training has arisen. Propofol usage seems to be increasing but it's still underused. It is a safe alternative for simple endoscopic procedures in low risk patients even if administered by non-anesthesiologists. Evidence on propofol safety in complex procedures and high risk patients is less robust and in these cases, the presence of an anesthetist should be considered. We review the existing evidence on the topic and evaluate the regional differences on sedation practices.

Psychopharmacological Profile of Hydroalcoholic Extract and P-Hydroxybenzoic Acid Obtained from <i>Bourreria huanita</i>(Boraginaceae) in Mice

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.

北五味子的镇静、催眠作用

目的对北五味子水提取物镇静、催眠药理作用进行初探。方法采用镇静、催眠实验观察北五味子水提取物对小鼠自主活动的影响 ,协同戊巴比妥钠对小鼠的催眠作用。结果北五味子水提取物能明显减少小鼠自主活动次数 ,增加阈下剂量戊巴比妥钠致小鼠睡眠只数 ,延长阈上剂量戊巴比妥钠致小鼠睡眠时间。结论北五味子水提取物有明显的镇静、催眠作用。

不同提取工艺酸枣仁汤的药效学研究

目的:通过药效学研究对酸枣仁汤剂提取工艺进行筛选。方法:观察不同提取工艺样品对小鼠自主活动和对阈上剂量戊巴比妥钠所致睡眠时间的影响。结果:酸枣仁汤水煎液和95％醇提液均有镇静、催眠作用。结论:选取酸枣仁汤水煎液为较优提取工艺。

南、北五味子提取物对小鼠镇静、催眠作用的影响

目的:研究并比较南、北五味子不同溶剂提取物对小鼠镇静、催眠作用的影响。方法:采用系统溶剂分离法,对南、北五味子进行系统提取,观察各组分对小鼠自主活动的影响及协同戊巴比妥钠对小鼠的催眠作用。结果:南、北五味子的醚提物和醇提物能显著减少小鼠自主活动次数,增加阈下剂量戊巴比妥钠致小鼠睡眠只数,延长阈上剂量戊巴比妥钠致小鼠睡眠时间。结论:南、北五味子镇静、催眠有效成分主要分布于醚提物和醇提物中;南、北五味子相比,北五味子的镇静作用稍好,而催眠作用相当。

氧化槐定碱对小鼠中枢神经系统的影响

目的 探讨氧化槐定碱对中枢神经系统的影响。方法 采用行为药理学方法观察并测定氧化槐定碱对阈剂量和阈下剂量戊巴比妥催眠作用的影响 ,对小鼠外观活动和自身活动的影响及对戊四氮惊厥的影响。结果 腹腔内注射氧化槐定碱 2 50 ,50 0 ,1 0 0 0mg/kg ,小鼠自发活动抑制率分别为 42 6 % ,57 2 %和 76 3% ,戊巴比妥钠入睡时间分别缩短 38 4% ,49 0 %和 39 7% ,而睡眠时间分别延长 1 72 % ,1 38%和 389% ,并能明显加强阈下剂量戊巴比妥钠的催眠作用。氧化槐定碱 50 0 ,1 0 0 0mg/kg不能对抗戊四氮引起的惊厥。结论 氧化槐定碱具有镇静、催眠等中枢抑制作用。

大安颗粒的镇静、催眠作用

目的考察大安颗粒对动物自发活动和对戊巴比妥钠催眠作用的影响,观察其潜在的镇静、催眠作用。方法观察小鼠ig给药后,自由走动的时间、举双前肢的次数及自由活动的次数,以及戊巴比妥钠的催眠剂量和阈剂量对小鼠睡眠的影响,与阴性对照组比较具显著性差异。结果小鼠1次ig大安颗粒(生药)60.3、40.5g·kg-1(高、中剂量组)后60、90min可明显减少其在XZ-4小鼠自由活动计数器内的活动次数,与阴性对照组比较有非常显著的差异(P<0.01)。ig高剂量后30、60、90、120min,与阴性对照组比较自由走动时间显著减少(P<0.01);小鼠举双前肢的次数亦明显减少,与阴性对照组比较亦有显著的差异(P<0.05);高、中剂量组小鼠的入睡时间明显缩短(P<0.01)、睡眠时间明显延长(P<0.05),高剂量组对ip阈下剂量戊巴比妥钠后的小鼠入睡只数也显著增加(P<0.05)。结论大安颗粒具明显的镇静和催眠及与戊巴比妥钠协同的作用。

蜘蛛香的中枢抑制作用

蜘蛛香水提物ｉｐ或ｉｇ能协同戊巴比妥钠对小鼠的镇静、催眠作用；抑制小鼠的自发活动；并能对抗硫代氨基脲诱发小鼠惊厥；对印防己毒素诱发的惊厥虽无明显影响，但能明显延长其诱发惊厥潜伏期，ｉｐ，ｉｇ能明显减少小鼠扭体次数。

氧化槐定碱和氧化苦参碱对小鼠中枢的抑制作用

目的 研究氧化槐定碱对中枢神经系统的影响。方法 采用行为药理学方法观察并测定氧化槐定碱和氧化苦参碱对阈剂量和阈下剂量戊巴比妥钠催眠作用的影响、对小鼠外观活动和自发活动的影响及对戊四氮致惊厥作用的影响。结果 ip 1/ 16、1/ 8、1/ 4LD50 剂量的氧化槐定碱和氧化苦参碱都能引起小鼠自发活动的减少(P <0 .0 5 ) ,戊巴比妥钠入睡时间缩短 (P <0 .0 5 ) ,睡眠时间延长 (P <0 .0 5 ) ,并能明显加强阈下剂量戊巴比妥钠的催眠作用 (P <0 .0 5 )。 1/ 4LD50 的氧化槐定碱和氧化苦参碱均不能对抗戊四氮致惊厥作用。结论 氧化槐定碱和氧化苦参碱均具有中枢抑制作用 ,表现为镇静催眠。同比剂量氧化槐定碱在对小鼠自主活动抑制 ,对阈下剂量戊巴比妥钠协同作用略强于氧化苦参碱 ,但氧化苦参碱对延长戊巴比妥钠睡眠时间略强于氧化槐定碱。

蛇床子催眠活性组分对小鼠镇静催眠、学习记忆及宿醉反应的影响

目的:研究蛇床子催眠活性组分(CHC)对小鼠的镇静催眠、学习记忆及宿醉反应的影响。方法:取小鼠60只,随机分为空白对照组(2%聚山梨酯80溶液)、地西泮组(6 mg/kg)和CHC高、中、低剂量组(520、260、130 mg/kg),每组12只,每天ig相应药物2次。观察给药1 d后各组小鼠的入睡潜伏期和睡眠持续时间、睡眠后自主活动次数和站立次数、避暗实验的避暗潜伏期和错误次数;给药16 d后各组小鼠进行定位航行实验和空间探索实验。结果:与空白对照组比较,地西泮组和CHC各剂量组小鼠睡眠持续时间均延长、睡前和醒后站立次数均减少;地西泮组小鼠睡前错误次数增加,醒后活动次数减少,逃避潜伏期延长,目标时间缩短,目标路程占比减少;CHC高剂量组小鼠睡前避暗潜伏期延长,以上差异均有统计学意义(P<0.05或P<0.01)。与地西泮组比较,CHC中、高剂量组小鼠睡眠持续时间均延长,醒后活动次数均增加;CHC低剂量组小鼠睡前活动次数减少;CHC各剂量组小鼠睡前错误次数均减少,以上差异均有统计学意义(P<0.05或P<0.01)。与睡前比较,空白对照组小鼠醒后避暗潜伏期延长,CHC各剂量组小鼠醒后活动次数均增加、醒后站立次数均减少、醒后避暗潜伏期延长(除中剂量组外),以上差异均有统计学意义(P<0.05)。其余指标差异均无统计学意义(P>0.05)。结论:CHC对小鼠有镇静催眠作用,但对其学习记忆几乎无影响,也没有宿醉反应。

益脑胶囊的药效学研究

目的 :探讨益脑胶囊对小鼠中枢神经系统的作用及其急性毒性药理作用。方法 :观察益脑胶囊对小鼠自主活动、阈下剂量戊巴比妥钠睡眠个数及耐缺氧、抗疲劳等作用 ,并与安神补脑液比较。结果 :益脑胶囊有明显抑制小鼠自主活动、增加阈下剂量戊巴比妥钠小鼠的入睡个数、耐缺氧、抗疲劳等作用 ,益脑胶囊 (3.6g/kg)组作用较安神补脑液 (1.2 g/kg)组明显强 ,二组比较有显著意义 (P <0 .0 1)。急性毒性试验证明 :益脑胶囊毒性很低 ,大、小鼠口服灌胃LD50 分别大于 18g/kg ,36 g/kg(合生药 12 0 ,2 40g/kg)。 结论 :益脑胶囊具有较好镇静、诱导催眠、耐缺氧、抗疲劳作用。

天王补心丸全方及方中缺桔梗对小鼠镇静催眠作用的影响

目的:探讨中药古方天王补心丸对小鼠中枢神经系统的药理影响及舟楫之剂桔梗在该方剂中的作用。方法:采用小鼠自发活动计数、延长戊巴比妥钠睡眠时间及抗惊厥试验等方法,观察天王补心丸方、缺桔梗的天王补心丸方、天王补心丸中臣药酸枣仁、酸枣仁与桔梗配伍及其桔梗单独使用时的镇静、催眠与抗惊厥作用。结果:天王补心丸有良好的镇静、催眠与抗惊厥作用,但该方去掉桔梗后,镇静、催眠与抗惊厥效果明显下降;天王补心丸中重要成分酸枣仁本身有较好的镇静催眠作用加上桔梗后效果得到加强,但不如天王补心丸全方,桔梗本身没有镇静、催眠与抗惊厥作用。结论:在天王补心丸方剂的配伍中,桔梗作为舟楫之剂确实能载药上浮,增强该方对中枢神经系统的作用。

灵芝生料酿制液镇静催眠作用的研究

目的考察灵芝生料酿制液(GLB)镇静催眠药理作用。方法取NIH小鼠连续灌胃0.06,0.12,0.24g/kgGLB15d,测定GLB对实验小鼠自发活动情况,对戊巴比妥钠阈下剂量、阈剂量小鼠睡眠时间和对戊四氮致小鼠惊厥的作用。结果GLB灌胃可减少小鼠自发活动,显著延长阈上剂量戊巴比妥钠致小鼠睡眠时间,增加阈下剂量戊巴比妥钠睡眠动物数,GLB与戊巴比妥钠有协同作用。有对抗戊四氮致惊厥发作的作用,且剂量越大,作用越明显。结论GLB有明显的镇静、催眠、抗惊厥等中枢抑制作用。

灵藤提取物对小鼠镇静催眠和免疫功能的影响

目的研究经灵芝发酵后的夜交藤提取物(简称灵藤提取物)对小鼠镇静催眠的作用和免疫功能的影响。方法观察灵藤提取物对小鼠自发活动,对戊巴比妥钠诱导小鼠睡眠时间和睡眠个数,以及对小鼠脾、胸腺器官和巨噬细胞吞噬能力的影响。结果灵藤提取物(5g/kg,10g/kg)能抑制小鼠的自发活动,延长戊巴比妥钠诱导的小鼠睡眠时间,增加小鼠睡眠个数,也能显著增加小鼠脾脏、胸腺的重量,增加巨噬细胞吞噬能力。结论灵藤提取物具有镇静催眠、提高免疫力的作用。

氧化槐定碱对小鼠中枢的抑制作用

目的 :探讨氧化槐定碱对中枢神经系统的影响。方法 :采用行为药理学方法观察并测定氧化槐定碱对阈剂量和阈下剂量戊巴比妥催眠作用的影响 ,对小鼠外观活动和自身活动的影响及对戊四氮惊厥的影响。结果 :ip氧化槐定碱 2 5 0、5 0 0、10 0 0mg·kg-1,小鼠自发活动抑制率分别为 4 2 6%、5 7 2 %、76 3 % ,戊巴比妥钠催眠后入睡时间分别缩短 3 8 4 %、4 9 0 %、3 9 7% ,而睡眠时间分别延长 172 %、13 8%、3 89% ,并能明显加强阈下剂量戊巴比妥钠的催眠作用。氧化槐定碱 5 0 0、10 0 0mg·kg-1不能对抗戊四氮引起的惊厥。结论 :氧化槐定碱具有镇静。

浅述半夏交通阴阳治不寐

不寐,本于阴阳不交。半夏,由阳入阴之药,能交通阴阳而治不寐。自《内经》开始,历代医家擅用半夏组方治疗不寐,且多主张重用之。现代药理学亦明确半夏及其复方具有镇静催眠之效。

氧化苦参碱对小鼠的中枢抑制作用

目的 :探讨氧化苦参碱对中枢神经系统的影响。方法 :采用行为药理学方法观察并测定氧化苦参碱对阈剂量和阈下剂量戊巴比妥纳催眠作用的影响 ,对小鼠外观活动和自发活动的影响及对戊四氮和最大电惊厥的影响。结果 :ip氧化苦参碱 5 0、10 0、2 0 0mg/kg小鼠自发活动抑制率分别为 5 4 3 %、43 0 %、71 0 % ,戊巴比妥钠入睡时间分别缩短 32 9%、32 9%、43 8% ,而睡眠时间分别延长 2 0 9 8%、42 1 2 %、6 86 8% ,并能明显加强阈下剂量戊巴比妥钠的催眠作用。氧化苦参碱 2 0 0、40 0mg/kgip均不能对抗戊四氮和最大电休克引起的惊厥。结论 :氧化苦参碱具有镇静。

合欢叶对小鼠镇静催眠作用的实验研究

目的揭示合欢叶的镇静催眠作用。方法以生理盐水为空白对照,观察小鼠灌胃药物后走动次数、举双前肢次数的变化情况,以及对戊巴比妥钠处理小鼠入睡时间和睡眠时间的影响。结果合欢叶低剂量(ig,31.6g/kg)能减少小鼠走动次数和举双前肢次数,能缩短戊巴比妥钠阈剂量给药小鼠的入睡时间,延长睡眠时间,与空白对照组相比差异显著(P<0.01);合欢叶高剂量(ig,79.0g/kg)能减少小鼠走动次数(P<0.05),能缩短戊巴比妥钠阈剂量给药小鼠的入睡时间,延长睡眠时间,与空白对照组相比差异显著(P<0.01)。结论合欢叶具有镇静催眠作用,且以低剂量为佳。