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Gabaa antagonist

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https://www.readbyqxmd.com/read/28339742/topiramate-modulates-post-infarction-inflammation-primarily-by-targeting-monocytes-or-macrophages
#1
Zhaohui Wang, Shiyuan Huang, Yuling Sheng, Xu Peng, Hui Liu, Nan Jin, Jun Cai, Yanwen Shu, Ting Li, Ping Li, Cheng Fan, Xiaofan Hu, Wenyong Zhang, Rui Long, Ya You, Caihong Huang, Yi Song, Chunhua Xiang, Jue Wang, Yong Yang, Kun Liu
Aims: Monocytes/macrophages response plays a key role in post-infarction inflammation that contributes greatly to post-infarction ventricular remodeling and cardiac rupture. Therapeutic targeting of the GABAA receptor, which is enriched in monocytes/macrophages but not expressed in the myocardium, may be possible after myocardial infarction. Methods and results: After MI was induced by ligation of the coronary artery, C57BL/6 mice were intraperitoneally administered with one specific agonist or antagonist of the GABAA receptor (topiramate or bicuculline), in the setting of presence or depletion of monocytes/macrophages...
February 17, 2017: Cardiovascular Research
https://www.readbyqxmd.com/read/28336918/clinically-applicable-gaba-receptor-positive-allosteric-modulators-promote-%C3%A3-cell-replication
#2
Jide Tian, Hoa Dang, Blake Middleton, Daniel L Kaufman
A key goal of diabetes research is to develop treatments to safely promote human ß-cell replication. It has recently become appreciated that activation of γ-aminobutyric acid receptors (GABA-Rs) on ß-cells can promote their survival and replication. A number of positive allosteric modulators (PAMs) that enhance GABA's actions on neuronal GABAA-Rs are in clinical use. Repurposing these GABAA-R PAMs to help treat diabetes is theoretically appealing because of their safety and potential to enhance the ability of GABA, secreted from ß-cells, or exogenously administered, to promote ß-cell replication and survival...
March 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28326934/activations-of-muscarinic-m1-receptors-in-the-anterior-cingulate-cortex-contribute-to-the-antinociceptive-effect-via-gabaergic-transmission
#3
Kohei Koga, Yu Matsuzaki, Kenji Honda, Fumihiro Eto, Tomonori Furukawa, Keisuke Migita, Keiichi Irie, Kenichi Mishima, Shinya Ueno
Background Cholinergic systems regulate the synaptic transmission resulting in the contribution of the nociceptive behaviors. Anterior cingulate cortex is a key cortical area to play roles in nociception and chronic pain. However, the effect of the activation of cholinergic system for nociception is still unknown in the cortical area. Here, we tested whether the activation of cholinergic receptors can regulate nociceptive behaviors in adult rat anterior cingulate cortex by integrative methods including behavior, immunohistochemical, and electrophysiological methods...
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/28320952/identification-of-a-putative-binding-site-critical-for-general-anesthetic-activation-of-trpa1
#4
Hoai T Ton, Thieu X Phan, Ara M Abramyan, Lei Shi, Gerard P Ahern
General anesthetics suppress CNS activity by modulating the function of membrane ion channels, in particular, by enhancing activity of GABAA receptors. In contrast, several volatile (isoflurane, desflurane) and i.v. (propofol) general anesthetics excite peripheral sensory nerves to cause pain and irritation upon administration. These noxious anesthetics activate transient receptor potential ankyrin repeat 1 (TRPA1), a major nociceptive ion channel, but the underlying mechanisms and site of action are unknown...
March 20, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28319848/treatment-of-premenstrual-dysphoric-disorder-with-the-gabaa-receptor-modulating-steroid-antagonist-sepranolone-uc1010-a-randomized-controlled-trial
#5
Marie Bixo, Karin Ekberg, Inger Sundström Poromaa, Angelica Lindén Hirschberg, Aino Fianu Jonasson, Lotta Andréen, Erika Timby, Marianne Wulff, Agneta Ehrenborg, Torbjörn Bäckström
CONTEXT: Allopregnanolone is a metabolite from progesterone and a positive modulator of the GABAA receptor. This endogenous steroid may induce negative mood in sensitive women when present in serum levels comparable to the premenstrual phase. Its endogenous isomer, isoallopregnanolone, has been shown to antagonize allopregnanolone effects in experimental animal and human models. OBJECTIVE: The objective was to test whether inhibition of allopregnanolone by treatment with the GABAA modulating steroid antagonist (GAMSA) Sepranolone (UC1010) during the premenstrual phase could reduce symptoms of the premenstrual dysphoric disorder (PMDD)...
March 1, 2017: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/28316587/characterization-of-the-antinociceptive-mechanisms-of-khat-extract-catha-edulis-in-mice
#6
Elham A Afify, Huda M Alkreathy, Ahmed S Ali, Hassan A Alfaifi, Lateef M Khan
This study investigated the antinociceptive mechanisms of khat extract (100, 200, and 400 mg/kg, i.p.) in four pain models: two thermic (hot plate, tail-flick) and two chemical (acetic acid, formalin) models. Male mice were pretreated intraperitoneally (i.p.) with the opioid receptor blocker naloxone (5 mg/kg), the cholinergic antagonist atropine (2 mg/kg), the selective α1 blocker prazosin (1 mg/kg), the dopamine D2 antagonist haloperidol (1.5 mg/kg), or the GABAA receptor antagonist, bicuculline (1 mg/kg) 15 minutes prior to i...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28292881/evidence-for-a-histaminergic-input-from-the-ventral-tuberomammillary-nucleus-to-the-solitary-tract-nucleus-involved-in-arterial-pressure-regulation
#7
Ko Yamanaka, Sabine S Gouraud, Miwa Takagishi, Akira Kohsaka, Masanobu Maeda, Hidefumi Waki
The tuberomammillary nucleus (TMN) of the posterior hypothalamus has a high density of histaminergic neurons, the projection fibers of which are present in many areas of the brain, including the nucleus tractus solitarius (NTS), which controls arterial pressure (AP). In this study, we investigated whether the TMN-NTS pathway is involved in central cardiovascular regulation. Bicuculline, a gamma-aminobutyric acid type A (GABAA) receptor antagonist, was microinjected into the ventral TMN of anesthetized rats and its effects on AP and heart rate (HR) were observed...
March 2017: Physiological Reports
https://www.readbyqxmd.com/read/28288863/toluene-s-effects-on-activity-and-extracellular-dopamine-in-the-mouse-are-altered-by-gabaa-antagonism
#8
Sean P Callan, Aaron K Apawu, Tiffany A Mathews, Scott E Bowen
The abuse of inhalants like toluene continues to be widespread around the world, especially among children and teenagers. Despite its frequency of misuse, the dynamics between dopamine (DA) and gamma-aminobutyric acid (GABA) in response to toluene exposure remains unclear. To further decipher toluene's actions, we used a dynamic exposure system in combination with microdialysis to examine in vivo the effects of acutely inhaled toluene on DA release within the mouse caudate putamen (CPu). Results show that toluene inhalation produced increases in DA levels and locomotor activity...
March 10, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28284708/visual-experience-regulates-the-development-of-long-term-synaptic-modifications-induced-by-low-frequency-stimulation-in-mouse-visual-cortex
#9
Taketoshi Sugimura, Mariko Yamamoto, Kazumasa Yamada, Yukio Komatsu, Yumiko Yoshimura
Manipulation of visual experience can considerably modify visual responses of visual cortical neurons even in adulthood in the mouse, although the modification is less profound than that observed during the critical period. Our previous studies demonstrated that low-frequency (2Hz) stimulation for 15min applied to layer 4 induces T-type Ca(2+) channel-dependent long-term potentiation (LTP) at excitatory synapses in layer 2/3 neurons of visual cortex during the critical period. In this study, we investigated whether low-frequency stimulation could induce synaptic plasticity in adult mice...
March 8, 2017: Neuroscience Research
https://www.readbyqxmd.com/read/28274653/effects-of-chemical-stimulation-of-the-lateral-wings-of-the-dorsal-raphe-nucleus-on-panic-like-defensive-behaviors-and-fos-protein-expression-in-rats
#10
Melina Matthiesen, Ailton Spiacci, Hélio Zangrossi
The lateral wings subnucleus of the dorsal raphe nucleus (lwDR) has been implicated in the modulation of panic-like behaviors, such as escape. Infusion of non- excitotoxic doses of the excitatory amino acid kainic acid into this subnucleus promptly evokes a vigorous escape response. In addition, rats exposed to panic-inducing situations show an increase in Fos protein expression in neurons within the lwDR. In the present study, we first investigated whether key structures associated with the mediation of escape behavior are recruited after chemical stimulation of the lwDR with kainic acid...
March 6, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28268105/prolonged-striatal-disinhibition-as-a-chronic-animal-model-of-tic-disorders
#11
Esther Vinner, Michal Israelashvili, Izhar Bar-Gad
BACKGROUND: Experimental findings and theoretical models have associated Tourette syndrome with abnormal striatal inhibition. The expression of tics, the hallmark symptom of this disorder, has been transiently induced in non-human primates and rodents by the injection of GABAA antagonists into the striatum, leading to temporary disinhibition. NEW METHOD: The novel chronic model of tic expression utilizes mini-osmotic pumps implanted subcutaneously in the rat back for prolonged infusion of bicuculline into the dorsolateral striatum...
March 4, 2017: Journal of Neuroscience Methods
https://www.readbyqxmd.com/read/28258626/glucose-concentrations-modulate-brain-derived-neurotrophic-factor-responsiveness-of-neurons-in-the-paraventricular-nucleus-of-the-hypothalamus
#12
William McIsaac, Alastair V Ferguson
The hypothalamic paraventricular nucleus (PVN) is critical for normal energy balance and has been shown to contain high levels of both BDNF and TrkB mRNA. Microinjections of BDNF into the PVN increase energy expenditure, suggesting BDNF plays an important role in energy homeostasis through direct actions in this nucleus. The current studies were undertaken to examine the postsynaptic effects of BDNF on the membrane potential of PVN neurons, and to determine if extracellular glucose concentrations modulated these effects...
March 4, 2017: Journal of Neuroendocrinology
https://www.readbyqxmd.com/read/28255983/vasopressin-v1a-receptors-mediate-the-hypertensive-effects-of-pyrnan-apelin-13-in-the-rat-rostral-ventrolateral-medulla
#13
Philip R Griffiths, Stephen J Lolait, Louise E Harris, Julian Fr Paton, Anne-Marie O'Carroll
Apelin is a ubiquitous peptide that can elevate arterial blood pressure (ABP) yet understanding of the mechanisms involved remain incomplete. Bilateral microinjection of [Pyr(1) ]apelin-13 into the rostral ventrolateral medulla (RVLM), a major source of sympathoexcitatory neurones, increases ABP and sympathetic nerve activity. We sought to investigate the potential involvement of neurotransmitter systems through which the apelin pressor response may occur within the RVLM. Adult male Wistar rats were anaesthetised and ABP was monitored via a femoral arterial catheter...
March 2, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28254772/central-inhibition-of-initiation-of-swallowing-by-systemic-administration-of-diazepam-and-baclofen-in-anaesthetized-rats
#14
Takanori Tsujimura, Shogo Sakai, Taku Suzuki, Izumi Ujihara, Kojun Tsuji, Jin Magara, Brendan J Canning, Makoto Inoue
Dysphagia is caused not only by neurological and/or structural damage but also by medication. We hypothesized memantine, dextromethorphan, diazepam and baclofen, all commonly used drugs with central sites of action, may regulate swallowing function. Swallows were evoked by upper airway (UA)/pharyngeal distension, punctate mechanical stimulation using a von Frey filament, capsaicin or distilled water (DW) applied topically to the vocal folds, and electrical stimulation of a superior laryngeal nerve (SLN) in anesthetized rats and were documented by recording electromyographic activation of the suprahyoid and thyrohyoid muscles and by visualizing laryngeal elevation...
March 2, 2017: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/28230208/optogenetic-activation-of-vglut2-expressing-excitatory-neurons-blocks-epileptic-seizure-like-activity-in-the-mouse-entorhinal-cortex
#15
Latefa Yekhlef, Gian Luca Breschi, Stefano Taverna
We investigated whether an anti-epileptic effect is obtained by selectively activating excitatory neurons expressing ChR2 under the promoter for the synaptic vesicular glutamate transporter 2 (VGLUT2). VGLUT2-expressing cells were optically stimulated while local field potential and whole-cell patch-clamp recordings were performed in mouse entorhinal cortical slices perfused with the proconvulsive compound 4-aminopyridine (4-AP). In control conditions, blue light flashes directly depolarized the majority of putative glutamatergic cells, which in turn synaptically excited GABAergic interneurons...
February 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28223240/carbachol-induced-network-oscillations-in-an-in-vitro-limbic-system-brain-slice
#16
Maxime Lévesque, Mauro Cataldi, Li-Yuan Chen, Shabnam Hamidi, Massimo Avoli
We employed simultaneous field potential recordings from CA3, subiculum and entorhinal cortex in an in vitro brain slice preparation to understand the involvement of these limbic areas in the generation of the field potential oscillations that are induced by bath application of the muscarinic receptor agonist carbachol. Regularly spaced oscillations that mainly presented at theta frequency range (5-12Hz) occurred synchronously in all three structures in the presence of carbachol. These oscillations, which disappeared when slices were perfused with pirenzepine or with glutamatergic receptor antagonists, were categorized as short (<4s) and long (>4s) with short events oscillating at higher frequencies than long events...
February 21, 2017: Neuroscience
https://www.readbyqxmd.com/read/28215510/short-term-treatment-with-flumazenil-restores-long-term-object-memory-in-a-mouse-model-of-down-syndrome
#17
Damien Colas, Bayarsaikhan Chuluun, Craig C Garner, H Craig Heller
Down syndrome (DS) is a common genetic cause of intellectual disability yet no pro-cognitive drug therapies are approved for human use. Mechanistic studies in a mouse model of DS (Ts65Dn mice) demonstrate that impaired cognitive function is due to excessive neuronal inhibitory tone. These deficits are normalized by chronic, short-term low doses of GABAA receptor (GABAAR) antagonists in adult animals, but none of the compounds investigated are approved for human use. We explored the therapeutic potential of flumazenil (FLUM), a GABAAR antagonist working at the benzodiazepine binding site that has FDA approval...
February 12, 2017: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/28163104/age-dependent-regulation-of-gaba-transmission-by-kappa-opioid-receptors-in-the-basolateral-amygdala-of-sprague-dawley-rats
#18
K R Przybysz, D F Werner, M R Diaz
Anxiety disorders are one of the most common and debilitating mental illnesses worldwide. Growing evidence indicates an age-dependent rise in the incidence of anxiety disorders from adolescence through adulthood, suggestive of underlying neurodevelopmental mechanisms. Kappa opioid receptors (KORs) are known to contribute to the development and expression of anxiety; however, the functional role of KORs in the basolateral amygdala (BLA), a brain structure critical in mediating anxiety, particularly across ontogeny, are unknown...
February 3, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28153485/loop-f-of-the-%C3%AE-subunit-determines-the-pharmacologic-profile-of-novel-competitive-inhibitors-of-gabaa-receptors
#19
Balázs Mihalik, Adrienn Pálvölgyi, Ferenc Bogár, Katalin Megyeri, István Ling, József Barkóczy, Ferenc Bartha, Tamás A Martinek, István Gacsályi, Ferenc A Antoni
The neurotransmitter γ-amino butyric acid (GABA) has a fundamental role in CNS function and ionotropic (GABAA) receptors that mediate many of the actions of GABA are important therapeutic targets. This study reports the mechanism of action of novel GABAA antagonists based on a tricyclic oxazolo-2,3-benzodiazepine scaffold. These compounds are orthosteric antagonists of GABA on heteropentameric GABAA receptors of αxβ2γ2 configuration expressed in HEK293 cells. In silico modelling predicted that the test compounds docked in the GABA binding-pocket and would interact with amino-acid residues in the α- and β-subunit interface that are known to be important for the binding of GABA...
January 31, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28150939/antinociceptive-effects-of-a-novel-%C3%AE-2-%C3%AE-3-subtype-selective-gabaa-receptor-positive-allosteric-modulator
#20
Lakeisha A Lewter, Janet L Fisher, Justin N Siemian, Kashi Reddy Methuku, Michael M Poe, James M Cook, Jun-Xu Li
Pain remains a challenging clinical condition and spinal GABAA receptors are crucial modulators of pain processing. α2/α3-subtype GABAA receptors mediate the analgesic actions of benzodiazepines. Positive allosteric modulators (PAMs) at α2/α3-subtype GABAA receptors may have analgesic potential. Here we report a new selective α2/α3-subtype GABAA receptor PAM in in vitro and in vivo pain assays. KRM-II-81 demonstrated similar efficacy at α1/α2/α3 GABAA receptors and negligible efficacy at α4/α5/α6 GABAA receptors, with α2 and α3-subtypes being 17- and 28-fold more potent than α1 subtypes in HEK-293T cells expressing GABAA receptors with different α subunits...
February 2, 2017: ACS Chemical Neuroscience
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