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https://www.readbyqxmd.com/read/29153631/human-abuse-potential-of-brivaracetam-in-healthy-recreational-central-nervous-system-depressant-users
#1
Kerri A Schoedel, Armel Stockis, Edward M Sellers
BACKGROUND: Brivaracetam is a new antiepileptic drug indicated for adjunctive treatment of focal seizures in adults at a dose of 50-200mg/day taken in two equal doses. The objective of this study was to evaluate the abuse potential of brivaracetam compared with alprazolam (positive control), placebo, and levetiracetam. METHODS: This was a randomized, double-blind, triple-dummy, crossover study in healthy male and female recreational central nervous system (CNS) depressant users aged 18-55years, who could distinguish between the subjective effects of alprazolam 2mg and placebo...
November 15, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/29150461/gabaa-receptor-activation-in-the-allosteric-coagonist-model-framework-relationship-between-ec50-and-basal-activity
#2
Gustav Akk, Daniel J Shin, Allison L Germann, Joseph H Steinbach
The concerted transition model for multimeric proteins is a simple formulation for analyzing the behavior of transmitter-gated ion channels. Here, we use the model to examine the relationship between the EC50 for activation of the GABAA receptor by the transmitter GABA and basal activity employing concatemeric ternary GABAA receptors expressed in Xenopus oocytes. The basal activity reflects receptor function in the absence of transmitter, and can be changed either by mutation to increase constitutive activity, or by addition of a second agonist (acting at a different site) to increase background activity...
November 17, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29147087/hydrolysate-preparation-with-high-content-of-5-hydroxytryptophan-from-liquid-egg-protein-and-its-sleep-potentiating-activity
#3
Jung Il Kwon, Yooheon Park, Sung Hee Han, Hyung Joo Suh
Alcalase hydrolysis of liquid egg white was used to produce 5-hydroxytryptophan (HTP) under various conditions and investigate the sleep-potentiating activity of liquid egg white hydrolysate (LEH) on pentobarbital-induced sleep. Alcalase hydrolysis yielded the highest content of 5-HTP (13.50 μg/mL), while neutrase hydrolysis showed the lowest 5-HTP content (5.23 μg/mL). The liquid egg white to water ratio (1:1) was optimal for the production of 5-HTP with high amino-nitrogen (A-N) content and degree of hydrolysis...
2017: Korean Journal for Food Science of Animal Resources
https://www.readbyqxmd.com/read/29105472/-effect-of-acupuncture-stimulation-of-different-acupoint-combinations-on-sleep-and-expression-of-circadian-clock-and-bmal-1-genes-in-hypothalamus-of-insomnia-rats
#4
Xin-Ran Wei, Gao-Wen Wei, Xue-Na Zheng, Xue-Fen Wu, Xiao-Li Chen, Li Liu, Qi-Qi Wen, Li-Na Xie, Zhi-Qiang Xie, Zeng-Hui Yue
OBJECTIVE: To observe the effect of manual acupuncture stimulation (MAS) of "Baihui"(GV 20)-"Shenmen"(HT 7)or GV 20-"Sanyinjiao"(SP 6) on sleep and expression of circadian rhythm genes (Clock and Bmal 1) in the hypothalamus in insomnia rats, so as to select a better acupoint group for insomnia. METHODS: A total of 53 SD rats were randomly divided into normal control (n=12),insomnia model (n=8), GV 20-HT 7(n=12), GV 20-SP 6(n=11),and GV 20-non-acupoint (n=10) groups...
October 25, 2017: Zhen Ci Yan Jiu, Acupuncture Research
https://www.readbyqxmd.com/read/29099542/chloral-hydrate-as-a-sedating-agent-for-neurodiagnostic-procedures-in-children
#5
REVIEW
Choong Yi Fong, Chee Geap Tay, Lai Choo Ong, Nai Ming Lai
BACKGROUND: Paediatric neurodiagnostic investigations, including brain neuroimaging and electroencephalography (EEG), play an important role in the assessment of neurodevelopmental disorders. The use of an appropriate sedative agent is important to ensure the successful completion of the neurodiagnostic procedures, particularly in children, who are usually unable to remain still throughout the procedure. OBJECTIVES: To assess the effectiveness and adverse effects of chloral hydrate as a sedative agent for non-invasive neurodiagnostic procedures in children...
November 3, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29081090/sinomenine-an-alkaloid-derived-from-sinomenium-acutum-potentiates-pentobarbital-induced-sleep-behaviors-and-non-rapid-eye-movement-nrem-sleep-in-rodents
#6
Jae Hyeon Yoo, Tae-Woo Ha, Jin Tae Hong, Ki-Wan Oh
Sinomenium acutum has been long used in the preparations of traditional medicine in Japan, China and Korea for the treatment of various disorders including rheumatism, fever, pulmonary diseases and mood disorders. Recently, it was reported that Sinomenium acutum, has sedative and anxiolytic effects mediated by GABA-ergic systems. These experiments were performed to investigate whether sinomenine (SIN), an alkaloid derived from Sinomenium acutum enhances pentobarbital-induced sleep via γ-aminobutyric acid (GABA)-ergic systems, and modulates sleep architecture in mice...
November 1, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/29077609/impact-of-anesthetic-regimen-on-remote-ischemic-preconditioning-in-the-rat-heart-in-vivo
#7
Friederike Behmenburg, Patrick van Caster, Sebastian Bunte, Timo Brandenburger, André Heinen, Markus W Hollmann, Ragnar Huhn
Remote ischemic preconditioning (RIPC) seems to be a promising cardioprotective strategy with contradictive clinical data suggesting the anesthetic regimen influencing the favorable impact of RIPC. This study aimed to investigate whether cardio protection by RIPC is abolished by anesthetic regimens. Male Wistar rats were randomized to 6 groups. Anesthesia was either maintained by pentobarbital (Pento) alone or a combination of sevoflurane (Sevo) and remifentanil or propofol (Prop) and remifentanil in combination with and without RIPC...
October 26, 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29061514/bold-mri-demonstrates-acute-placental-and-fetal-organ-hypoperfusion-with-fetal-brain-sparing-during-hypercapnia
#8
Yehuda Ginosar, Yuval Gielchinsky, Nathalie Nachmansson, Lital Hagai, Joel Shapiro, Uriel Elchalal, Rinat Abramovitch
INTRODUCTION: We evaluated changes in placental and fetal hemodynamics in rodents during acute hypercapnia using BOLD-MRI and Doppler ultrasound. METHODS: Animals were anesthetized with pentobarbital and, in consecutive 4-min periods, breathed: air, 21%O2:5%CO2, and 95%O2:5%CO2. BOLD-MRI: Pregnant ICR mice (n = 6; E17.5) were scanned in a 4.7-T Bruker Biospec spectrometer. Placenta and fetal liver, heart and brain were identified on True-FISP images...
September 11, 2017: Placenta
https://www.readbyqxmd.com/read/28975098/the-protective-effect-of-buffalo-s-milk-against-toluene-induced-nephrotoxicity-in-rats
#9
Maryam Afravy, Kambiz Angali, Ali Khodadadi, Massumeh Ahmadizadeh
BACKGROUND: Toluene is widely used in different activities of industrial, commercial and household applications. It can cause damage to the human body. Buffalos' milk has a good nutritive value. OBJECTIVES: The aim of this study is to examine the negative effects of toluene on kidney tissues and to investigate the protective effects of buffalo's milk against toluene-induced nephrotoxicity in rats. MATERIALS AND METHODS: Forty adult male Wistar rats (180-220 g weight) were randomly assigned to eight groups (n = 5)...
July 2017: Journal of Nephropathology
https://www.readbyqxmd.com/read/28975097/ameliorative-effect-of-vitamin-e-on-trichloroethylene-induced-nephrotoxicity-in-rats
#10
Mojgan Heydari, Massumeh Ahmadizadeh, Kambiz Ahmadi Angali
BACKGROUND: 1,1,2-Trichloroethylene (TCE) is an important organic solvent which is widespread in the environment. Work place exposure to TCE has been associated adverse effects in many organs including kidney. Vitamin E is an antioxidant that can overcome oxidative stress. OBJECTIVES: The aim of the present study is to examine the role of vitamin E against destructive effects of TCE on rat kidney. MATERIALS AND METHODS: A total of 35 male Wistar rats were randomly divided into seven groups of equal number in each...
July 2017: Journal of Nephropathology
https://www.readbyqxmd.com/read/28969235/super-refractory-status-epilepticus-a-therapeutic-challenge-in-paediatrics
#11
Shrikiran Aroor, Kanaparthi Shravan, Suneel C Mundkur, C Jayakrishnan, Sai Sripad Rao
A status epilepticus which persists for 24 hours or more after starting treatment with anaesthesia or has recurred inspite of general anaesthesia is known as Super-Refractory Status Epilepticus (SRSE). It includes cases where status epilepticus recurs on reduction or withdrawal of anaesthesia. SRSE, though infrequently seen, constitutes a medical emergency due to the associated high morbidity and mortality. No clear cut guidelines are available till date for the management of SRSE. Most of the published literature was case reports and expert opinion...
August 2017: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/28941387/management-protocols-for-status-epilepticus-in-the-pediatric-emergency-room-systematic-review-article
#12
REVIEW
Cheuk C Au, Ricardo G Branco, Robert C Tasker
OBJECTIVE: This systematic review of national or regional guidelines published in English aimed to better understand variance in pre-hospital and emergency department treatment of status epilepticus. SOURCES: Systematic search of national or regional guidelines (January 2000 to February 2017) contained within PubMed and Google Scholar databases, and article reference lists. The search keywords were status epilepticus, prolonged seizure, treatment, and guideline...
November 2017: Jornal de Pediatria
https://www.readbyqxmd.com/read/28936180/mouse-anaphylactic-hypotension-is-characterized-by-initial-baroreflex-independent-renal-sympathoinhibition-followed-by-sustained-renal-sympathoexcitation
#13
Tao Zhang, Mamoru Tanida, Kunitoshi Uchida, Yoshiro Suzuki, Wei Yang, Yuhichi Kuda, Yasutaka Kurata, Makoto Tominaga, Toshishige Shibamoto
Aim: The hemodynamic response to mouse systemic anaphylaxis is characterized by an initial hypertension followed by sustained hypotension. However, the defense mechanisms of the sympathetic nervous system against this circulatory disturbance is not known. Here, we investigated the renal sympathetic nerve activity (RSNA) response to mouse systemic anaphylaxis, along with the roles of carotid sinus baroreceptor, vagal nerves and the transient receptor potential vanilloid type 1 channel (TRPV1). Methods: Male ovalbumin-sensitized C57BL/6N mice were used under pentobarbital anesthesia...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28916246/pre-clinical-toxicology-considerations-for-vaccine-development
#14
REVIEW
Nabil Al-Humadi
Vaccine development requires pre-clinical toxicology studies, following good laboratory practice (GLP), before first in human (phase I) use. Many factors are critical in the final outcome of any pre-clinical toxicology study. The study design is one of these critical factors and should be carefully planned to avoid any false negative and/or false positive results. Preparation is another most critical factor in a successful study. Major changes in any procedure during the course of study should be avoided by all means...
September 12, 2017: Vaccine
https://www.readbyqxmd.com/read/28911622/sedative-and-hypnotic-effects-of-supercritical-carbon-dioxide-fluid-extraction-from-schisandra-chinensis-in-mice
#15
Hongyan Zhu, Lina Zhang, Guoli Wang, Zhongmei He, Yan Zhao, Yonghua Xu, Yugang Gao, Lianxue Zhang
Schisandra chinensis is a traditional Chinese medicine that has been used for treating insomnia and neurasthenia for centuries. Lignans, which are considered to be the bioactive components, are apt to be extracted by supercritical carbon dioxide. This study was conducted to investigate the sedative and hypnotic activities of the supercritical carbon dioxide fluid extraction of S. chinensis (SFES) in mice and the possible mechanisms. SFES exhibited an obvious sedative effect on shortening the locomotor activity in mice in a dose-dependent (10-200 mg/kg) manner...
October 2016: Journal of Food and Drug Analysis
https://www.readbyqxmd.com/read/28905718/physiologic-behavioral-and-histologic-responses-to-various-euthanasia-methods-in-c57bl-6ntac-male-mice
#16
Gregory P Boivin, Michael A Bottomley, Patricia A Schiml, Lori Goss, Nadja Grobe
Rodent euthanasia using exposure to increasing concentrations of CO2 has come under scrutiny due to concerns of potential pain during the euthanasia process. Alternatives to CO2, such as isoflurane and barbiturates, have been proposed as more humane methods of euthanasia. In this study, we examined 3 commonly used euthanasia methods in mice: intraperitoneal injection of pentobarbital-phenytoin solution, CO2 inhalation, and isoflurane anesthesia followed by CO2 inhalation. We hypothesized that pentobarbital-phenytoin euthanasia would cause fewer alterations in cardiovascular response, result in less behavioral evidence of pain or stress, and produce lower elevations in ACTH than would the isoflurane and CO2 methods, which we hypothesized would not differ in regard to these parameters...
January 1, 2017: Journal of the American Association for Laboratory Animal Science: JAALAS
https://www.readbyqxmd.com/read/28902674/disruption-of-hippocampal-multisynaptic-networks-by-general-anesthetics
#17
Min-Ching Kuo, L Stan Leung
BACKGROUND: Previous studies showed that synaptic transmission is affected by general anesthetics, but an anesthetic dose response in freely moving animals has not been done. The hippocampus provides a neural network for the evaluation of isoflurane and pentobarbital on multisynaptic transmission that is relevant to memory function. METHODS: Male Long-Evans rats were implanted with multichannel and single electrodes in the hippocampus. Spontaneous local field potentials and evoked field potentials were recorded in freely behaving rats before (baseline) and after various doses of isoflurane (0...
November 2017: Anesthesiology
https://www.readbyqxmd.com/read/28884085/anti-anxiety-and-hypnotic-effects-of-ethanolic-and-aqueous-extracts-of-lippia-citriodora-leaves-and-verbascoside-in-mice
#18
Bibi Marjan Razavi, Naser Zargarani, Hossein Hosseinzadeh
OBJECTIVES: The extract of Lippia citriodora and its main component, verbascoside, are known for their hypnotic effects in traditional medicine. In this study, the anxiolytic and hypnotic effects of L. citriodora leave extracts and verbascoside were evaluated in mice. MATERIALS AND METHODS: Animals were divided into 11 groups of six mice each. Group I received normal saline, Group II received Diazepam (2 mg/kg) as positive control, Groups III, IV and V received L...
July 2017: Avicenna Journal of Phytomedicine
https://www.readbyqxmd.com/read/28864241/theacrine-a-purine-alkaloid-from-camellia-assamica-var-kucha-with-a-hypnotic-property-via-the-adenosine-system
#19
Haoyi Qiao, Xiansheng Ye, Xiaoyu Bai, Jun He, Tingli Li, Jia Zhang, Weiku Zhang, Jiekun Xu
Theacrine (l,3,7,9-tetramethyluric acid), a purine alkaloid from Camellia assamica var. kucha, has diverse pharmacological properties, including sedative and hypnotic activities, anti-inflammatory and analgesic activities, antidepressant effects, and a protective effect against stress-provoked liver damage. The present study aims to investigate the possible mechanism of the hypnotic activity of theacrine. The results revealed that theacrine significantly enhanced pentobarbital-induced sleep at a dose of 3.0mg/kg (i...
October 17, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28857763/competitive-antagonism-of-anesthetic-action-at-the-%C3%AE-aminobutyric-acid-type-a-receptor-by-a-novel-etomidate-analog-with-low-intrinsic-efficacy
#20
Celena Ma, Ervin Pejo, Megan McGrath, Selwyn S Jayakar, Xiaojuan Zhou, Keith W Miller, Jonathan B Cohen, Douglas E Raines
BACKGROUND: The authors characterized the γ-aminobutyric acid type A receptor pharmacology of the novel etomidate analog naphthalene-etomidate, a potential lead compound for the development of anesthetic-selective competitive antagonists. METHODS: The positive modulatory potencies and efficacies of etomidate and naphthalene-etomidate were defined in oocyte-expressed α1β3γ2L γ-aminobutyric acid type A receptors using voltage clamp electrophysiology. Using the same technique, the ability of naphthalene-etomidate to reduce currents evoked by γ-aminobutyric acid alone or γ-aminobutyric acid potentiated by etomidate, propofol, pentobarbital, and diazepam was quantified...
November 2017: Anesthesiology
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