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Xiaoyu Hu, Xuebi Tian, Xiao Guo, Ying He, Haijun Chen, Jia Zhou, Zaijie Jim Wang
Development of opioid tolerance and dependence hinders the use of opioids for the treatment of chronic pain. In searching for the mechanism and potential intervention for opioid tolerance and dependence, we studied the action of two positive allosteric modulators of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR PAMs). In mice treated with morphine (100 mg/kg, s.c.), acute morphine tolerance and dependence developed in 4-6 h. Treatment with aniracetam, a well-established AMPAR PAM, was able to completely prevent and reverse the development of acute antinociceptive tolerance to morphine...
April 25, 2018: Neuropharmacology
Cheng-Hwang Perng, Yue-Cune Chang, Ruu-Fen Tzang
OBJECTIVE: No cure is currently available for dementia; however, various treatments and interventions have been reported to be effective. The factors influencing the efficacy of dementia treatment have not been comprehensively evaluated. This study evaluated the factors influencing treatment effects on cognitive dysfunction in dementia by comparing the results obtained from a meta-analysis based on meta-regression. METHODS: We searched for articles, clinical trials, and meta-analyses on the efficacy of pharmacotherapy or psychosocial treatment for dementia published between 2000 and 2016 in the MEDLINE/PubMed, Cochrane Library, SCOPUS, and Airiti Library databases...
May 2018: Psychopharmacology
Qingxia Kong, Xia Min, Ran Sun, Jianying Gao, Ruqing Liang, Lei Li, Xu Chu
The present study aimed to investigate the effects of various pharmacological agents on the hippocampal expression of neural cell adhesion molecule 1 (NCAM1) and extracellular signal-regulated kinase 2 (ERK2) in epileptic rats with cognitive dysfunction. The experiments were conducted using 120 Wistar rats: 20 controls and 100 with pilocarpine-induced status epilepticus (SE). The SE rats were randomly assigned to 5 groups (n=20/group) that received daily treatments for 1 month with one of the following: (i) saline (no effect on epilepsy); (ii) carbamazepine (an anticonvulsant); (iii) oxcarbazepine (an anticonvulsant); (iv) aniracetam (a nootropic); or (v) donepezil (an acetylcholinesterase inhibitor)...
September 2016: Oncology Letters
Manuela Eisenhardt, Sarah Leixner, Rafael Luján, Rainer Spanagel, Ainhoa Bilbao
UNLABELLED: Glutamatergic input within the mesolimbic dopamine (DA) pathway plays a critical role in the development of addictive behavior. Although this is well established for some drugs of abuse, it is not known whether glutamate receptors within the mesolimbic system are involved in mediating the addictive properties of chronic alcohol use. Here we evaluated the contribution of mesolimbic NMDARs and AMPARs in mediating alcohol-seeking responses induced by environmental stimuli and relapse behavior using four inducible mutant mouse lines lacking the glutamate receptor genes Grin1 or Gria1 in either DA transporter (DAT) or D1R-expressing neurons...
November 25, 2015: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
William F Borschel, Kirstie A Cummings, LeeAnn K Tindell, Gabriela K Popescu
Among glutamate-gated channels, NMDA receptors produce currents that subside with unusually slow kinetics, and this feature is essential to the physiology of central excitatory synapses. Relative to the homologous AMPA and kainate receptors, NMDA receptors have additional intersubunit contacts in the ligand binding domain that occur at both conserved and non-conserved sites. We examined GluN1/GluN2A single-channel currents with kinetic analyses and modeling to probe these class-specific intersubunit interactions for their role in glutamate binding and receptor gating...
October 30, 2015: Journal of Biological Chemistry
Haoquan Li, Kaiwu Dong, Helfried Neumann, Matthias Beller
Carbonylation reactions allow the efficient synthesis of all kinds of carbonyl-containing compounds. Here, we report a straightforward synthesis of various imides from olefins and CO for the first time. The established hydroamidocarbonylation reaction affords imides in good yields (up to 90 %) and with good regioselectivity (up to 99:1) when applying different alkenes and amides. The synthetic potential of the method is highlighted by the synthesis of Aniracetam by intramolecular hydroamidocarbonylation.
August 24, 2015: Angewandte Chemie
Rong-lin Cai, Hong-liang Cheng, Ting Zhou, Guo-qing Chen, Xing-sheng Chen, Sheng-bing Wu
OBJECTIVE: To observe the effect of electroacupuncture (EA) of "Dazhui" (GV 14), "Baihui" (GV 20), etc. on learning-memory ability and expression of vascular endothelial growth factor (VEGF) mRNA, VEGF receptor 1 (VEGFR-1/Flt-1) mRNA, and VEGFR-2 (Flk-1) mRNA in the hippocampus in vascular cognitive impairment (VCI) rats so as to reveal its mechanism underlying improvement of VCI. METHODS: A total of 60 Wistar rats were randomly divided into sham operation, VCI model, EA and medication groups (n=12 in each group)...
February 2015: Zhen Ci Yan Jiu, Acupuncture Research
Lorenz Deutschenbaur, Johannes Beck, Anna Kiyhankhadiv, Markus Mühlhauser, Stefan Borgwardt, Marc Walter, Gregor Hasler, Daniel Sollberger, Undine E Lang
Major depression is a common, recurrent mental illness that affects millions of people worldwide. Recently, a unique fast neuroprotective and antidepressant treatment effect has been observed by ketamine, which acts via the glutamatergic system. Hence, a steady accumulation of evidence supporting a role for the excitatory amino acid neurotransmitter (EAA) glutamate in the treatment of depression has been observed in the last years. Emerging evidence indicates that N-methyl-D-aspartate (NMDA), group 1 metabotropic glutamate receptor antagonists and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) agonists have antidepressant properties...
January 4, 2016: Progress in Neuro-psychopharmacology & Biological Psychiatry
Jie-Feng Cui, Wei Yang, Yan-Ming Xie, Yong Sun, Yan Zhuang, Yong-Yan Wang
This study aims to explore and analyze the condition of concurrent diseases and medicine use of traditional Chinese medicine (TCM) and western medicine among the patients with insomnia. One thousand and sxity seven cases of data from 20 national hospitals' hospital information system (HIS) databases were collected. The frequent concurrent diseases included hypertension (26.9%), brain blood supply insufficiency (24.93%), cerebral infarction (19.49%), blood lipoprotein disturbance (15.28%), coronary heart disease (14...
September 2014: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Thomas W Elston, Ashvini Pandian, Gregory D Smith, Andrew J Holley, Nanjing Gao, Joaquin N Lugo
There is a growing community of individuals who self-administer the nootropic aniracetam for its purported cognitive enhancing effects. Aniracetam is believed to be therapeutically useful for enhancing cognition, alleviating anxiety, and treating various neurodegenerative conditions. Physiologically, aniracetam enhances both glutamatergic neurotransmission and long-term potentiation. Previous studies of aniracetam have demonstrated the cognition-restoring effects of acute administration in different models of disease...
2014: PloS One
Si-Kang Li, Ding-Ming Ding, Zheng-Long Zhang, Lan Ma, Hai-Yan Huang, Xiao-Hong Wu
OBJECTIVE: To compare the therapeutic differences among scalp acupuncture combined with auricular point sticking, body acupuncture and western medication for treatment of vascular dementia (VD). METHODS: Ninety cases were randomly divided into a combined therapy group (31 cases), a body acupuncture group (29 cases) and a western medication group (30 cases). The combined therapy group was treated with scalp acupuncture at forehead middle line, parieral middle line, temporal front line and temporal rear line as well as auricular point sticking at naogan (AT3,41), shen (CO10), shenmen (TF4), zhen (AT3), once a day; the body acupuncture group was treated with acupuncture at Baihui (GV 20), Fengchi (GB 20), Zusanli (ST 36) and so on, once a day; the western medication group was treated with oral administration of aniracetam tablets, 0...
May 2014: Zhongguo Zhen Jiu, Chinese Acupuncture & Moxibustion
Junjie Bian, Zhixiang Yuan, Xiaoliang Chen, Yuan Gao, Chaoqun Xu, Jianyou Shi
PURPOSE: To prepare a mixture of multiple-coated aniracetam nasal polylactic-acid nanoparticles (M-C-PLA-NP) and evaluate its stability preliminarily in vitro and its brain-targeting efficiency in vivo. METHODS: The solvent diffusion-evaporation combined with magnetic stirring method has been chosen for the entrapment of aniracetam. The M-C-PLA-NP was characterized with respect to its morphology, particle size, size distribution and aniracetam entrapment efficiency...
2016: Drug Delivery
Vik V Iasnetsov, I N Krylova
It has been established in experiments in rats that some nootropic substances (oxyracetam, aniracetam, nooglutil, mexidol, new 3-hydroxypyridine derivative SK-170, piracetam and noopept) produce marked antiamnestic effect on various models of amnesia (induced by microwave irradiation, acute hypoxia, and motion sickness). At the same time, meclophenoxate exhibited antiamnestic effect in the first and second models of amnesia, while 9-aminoacridine derivative HTOS-404 was only effective in the model of amnesia caused by microwave irradiation...
2013: Eksperimental'naia i Klinicheskaia Farmakologiia
Francisco Paulino Dubiela, Claudio Marcos Queiroz, Karin Di Monteiro Moreira, Jose N Nobrega, Luciane Valéria Sita, Sergio Tufik, Debora Cristina Hipolide
The present study addressed the effects of sleep deprivation (SD) on AMPA receptor (AMPAR) binding in brain regions associated with learning and memory, and investigated whether treatment with drugs acting on AMPAR could prevent passive avoidance deficits in sleep deprived animals. [(3)H]AMPA binding and GluR1 in situ hybridization signals were quantified in different brain regions of male Wistar rats either immediately after 96 h of sleep deprivation or after 24h of sleep recovery following 96 h of sleep deprivation...
November 15, 2013: Behavioural Brain Research
Christian Krintel, Kasper Harpsøe, Linda G Zachariassen, Dan Peters, Karla Frydenvang, Darryl S Pickering, Michael Gajhede, Jette S Kastrup
Positive allosteric modulators of the ionotropic glutamate receptor A2 (GluA2) can serve as lead compounds for the development of cognitive enhancers. Several benzamide-type (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor modulators such as aniracetam, CX516 and CX614 have been shown to inhibit the deactivation of AMPA receptors with a less pronounced effect on desensitization. Despite CX516 being an extensively investigated AMPA receptor modulator and one of the few clinically evaluated compounds, the binding mode of CX516 to AMPA receptors has not been reported...
September 2013: Acta Crystallographica. Section D, Biological Crystallography
Guo-Wei Zhang, Wei Zou, Fang Liu
OBJECTIVE: To observe the effects of the scalp acupuncture at Baihui (DU20) through Qubin (GB7) on the expressions of glial cell line-derived neurotrophic factor (GDNF) and vascular endothelial growth factor (VEGF) in the brain tissue of rats with acute intracerebral hemorrhage (AICH). METHODS: Totally 150 healthy male Wistar rats were used to prepare the intracerebral hemorrhage (ICH) model. They were randomly divided into the model group, the acupuncture group, and the Western medicine group, 50 in each group...
September 2012: Chinese Journal of Integrated Traditional and Western Medicine
Reginald Cannady, Kristen R Fisher, Brandon Durant, Joyce Besheer, Clyde W Hodge
Long-term alcohol exposure produces neuroadaptations that contribute to the progression of alcohol abuse disorders. Chronic alcohol consumption results in strengthened excitatory neurotransmission and increased α-amino-3-hydroxyl-5-methyl-4-isoxazole-propionate receptors (AMPA) receptor signaling in animal models. However, the mechanistic role of enhanced AMPA receptor activity in alcohol-reinforcement and alcohol-seeking behavior remains unclear. This study examined the role of enhanced AMPA receptor function using the selective positive allosteric modulator, aniracetam, in modulating operant alcohol self-administration and cue-induced reinstatement...
January 2013: Addiction Biology
Ying Xie, Xi Huang, Sui-yu Hu, Ying-jin Zhang, Yang Wang, Xin-jian Qiu, Ping Ren, Rong Fan, Chun-hu Zhang, Wei-bin Xie, Hui Ji, Juan He, Xiao Chen, Linhong Xie, Zhao-qian Liu, Hong-hao Zhou
It was recently discovered that ketamine can relieve depression in a matter of hours through an action on α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors. This is much more rapid than the several weeks required for the available antidepressants to show therapeutic efficacy. However, ketamine has negative side effects. The aim of this study was to determine whether the natural prokinetic drug meranzin hydrate (MH) has a fast-acting antidepressant effect mediated by AMPA receptors. By means of in vivo and in vitro experiments, we found that (1) treatment of rats with MH at 9 mg/kg decreased immobility time in a forced swimming test (FST), as did the popular antidepressant fluoxetine and the AMPA receptor positive modulator aniracetam...
February 2013: Amino Acids
Shuang Cai, Lei Wang
A simple and rapid high-performance liquid chromatography-electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS) method has been developed and validated for the determination of 4-p-anisamidobutyric acid (ABA; or N-anysoyl-γ-aminobutiryc acid, N-anisoyl-GABA), a major active metabolite of aniracetam, in human plasma. After protein precipitation of plasma sample with methanol, ABA and the internal standard lisinopril were separated on a Venusil ASB C₁₈ column at 25 °C. The mobile phase consisted of methanol-ammonium acetate (10 mmol/L) (30:70, v/v)...
May 15, 2012: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Pin Wang, Jing-Yi Tang, Jun Yang
OBJECTIVE: To observe the expression levels of hippocampal vascular endothelial growth factor (VEGF), fms-like tyrosine kinase-1 (flt-1), basic fibroblast growth factor (bFGF), and basic fibroblast growth factor receptor (bFGF-r) in vascular dementia (VD) rats, thus studying the angiogenesis mechanism of moxibustion in VD. METHODS: Sixty male elderly Wistar rats were selected. The VD rat model was prepared by bilateral carotid artery occlusion and reperfusion of sodium nitroprusside injection...
January 2012: Chinese Journal of Integrated Traditional and Western Medicine
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