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https://www.readbyqxmd.com/read/27933950/structure-activity-relationship-drug-metabolism-and-pharmacokinetics-properties-optimization-and-in-vivo-studies-of-new-brain-penetrant-triple-t-type-calcium-channel-blockers
#1
Romain Siegrist, Davide Pozzi, Gaël Jacob, Caterina Torrisi, Kilian Colas, Bertrand Braibant, Jacques Mawet, Thomas Pfeifer, Ruben de Kanter, Catherine Roch, Melanie Kessler, Olivier Corminboeuf, Olivier Bezençon
Despite the availability of numerous antiepileptic drugs, 20-30% of epileptic patients are pharmacoresistant with seizures not appropriately controlled. Consequently, new strategies to address this unmet medical need are required. T-type calcium channels play a key role in neuronal excitability and burst firing, and selective triple T-type calcium channel blockers could offer a new way to treat various CNS disorders, in particular epilepsy. Herein we describe the identification of new 1,4-benzodiazepines as brain penetrant and selective triple T-type calcium channel blockers...
December 8, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27932863/non-imidazole-based-histamine-h3-receptor-antagonists-with-anticonvulsant-activity-in-different-seizure-models-in-male-adult-rats
#2
Bassem Sadek, Ali Saad, Gniewomir Latacz, Kamil Kuder, Agnieszka Olejarz, Tadeusz Karcz, Holger Stark, Katarzyna Kieć-Kononowicz
A series of twelve novel non-imidazole-based ligands (3-14) was developed and evaluated for its in vitro binding properties at the human histamine H3 receptor (hH3R). The novel ligands were investigated for their in vivo protective effects in different seizure models in male adult rats. Among the H3R ligands (3-14) tested, ligand 14 showed significant and dose-dependent reduction in the duration of tonic hind limb extension in maximal electroshock (MES)-induced seizure model subsequent to acute systemic administration (5, 10, and 20 mg/kg, intraperitoneally), whereas ligands 4, 6, and 7 without appreciable protection in MES model were most promising in pentylenetetrazole (PTZ) model...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27932305/scavenging-of-highly-reactive-gamma-ketoaldehydes-attenuates-cognitive-dysfunction-associated-with-epileptogenesis
#3
Jennifer N Pearson, Eric Warren, Li-Ping Liang, L Jackson Roberts, Manisha Patel
Cognitive dysfunction is a major comorbidity of the epilepsies; however, treatments targeting seizure-associated cognitive dysfunction, particularly deficits in learning and memory are not available. Isoketals and neuroketals, collectively known as gamma-ketoaldehydes are formed via the non-enzymatic, free radical catalyzed oxidation of arachidonic acid and docosahexaenoic acid, respectively. They are attractive candidates for oxidative protein damage and resultant cognitive dysfunction due to their formation within the plasma membrane and their high proclivity to form cytotoxic adducts on protein lysine residues...
December 5, 2016: Neurobiology of Disease
https://www.readbyqxmd.com/read/27932302/hippocampal-asymmetry-differences-in-the-left-and-right-hippocampus-proteome-in-the-rat-model-of-temporal-lobe-epilepsy
#4
Leila Sadeghi, Albert Anatolyevich Rizvanov, Ilnur Ildusovich Salafutdinov, Bahareh Dabirmanesh, Mohammad Sayyah, Yaghoub Fathollahi, Khosro Khajeh
: The hippocampus is a complex brain structure and undergoes severe sclerosis and gliosis in temporal lobe epilepsy (TLE) as the most common type of epilepsy. The key features of the TLE may be reported in chronic animal models of epilepsy, such as pilocarpine model. Therefore, the current study was conducted in a rat pilocarpine model of acquired epilepsy. Two-dimensional gel electrophoresis based proteomic technique was used to compare the proteome map of the left and right hippocampus in both control and epileptic rats...
December 5, 2016: Journal of Proteomics
https://www.readbyqxmd.com/read/27918641/evaluation-of-the-biocompatibility-of-polypyrrole-implanted-subdurally-in-gaers
#5
Sebastien H Bauquier, Karen J McLean, Jonathan L Jiang, Ray C Boston, Alan Lai, Zhilian Yue, Simon E Moulton, Amy J Halliday, Gordon Wallace, Mark J Cook
This blinded controlled prospective randomized study investigates the biocompatibility of polypyrrole (PPy) polymer that will be used for intracranial triggered release of anti-epileptic drugs (AEDs). Three by three millimeters PPy are implanted subdurally in six adult female genetic absence epilepsy rats from Strasbourg. Each rat has a polymer implanted on one side of the cortex and a sham craniotomy performed on the other side. After a period of seven weeks, rats are euthanized and parallel series of coronal sections are cut throughout the implant site...
December 5, 2016: Macromolecular Bioscience
https://www.readbyqxmd.com/read/27917314/pentylenetetrazole-induced-seizures-in-developing-rats-prenatally-exposed-to-valproic-acid
#6
Angel A Puig-Lagunes, Jorge Manzo, Luis Beltrán-Parrazal, Consuelo Morgado-Valle, Rebeca Toledo-Cárdenas, Maria-Leonor López-Meraz
BACKGROUND: Epidemiological evidence indicates epilepsy is more common in patients with autism spectrum disorders (ASD) (20-25%) than in the general population. The aim of this project was to analyze seizure susceptibility in developing rats prenatally exposed to valproic acid (VPA) as autism model. METHODS: Pregnant females were injected with VPA during the twelfth embryonic day. Seizures were induced in fourteen-days-old rat pups using two models of convulsions: pentylenetetrazole (PTZ) and lithium-pilocarpine (Li-Pilo)...
2016: PeerJ
https://www.readbyqxmd.com/read/27909008/trajectory-of-parvalbumin-cell-impairment-and-loss-of-cortical-inhibition-in-traumatic-brain-injury
#7
Tsung-Hsun Hsieh, Henry Hing Cheong Lee, Mustafa Qadir Hameed, Alvaro Pascual-Leone, Takao K Hensch, Alexander Rotenberg
Many neuropsychiatric symptoms that follow traumatic brain injury (TBI), including mood disorders, sleep disturbance, chronic pain, and posttraumatic epilepsy (PTE) are attributable to compromised cortical inhibition. However, the temporal trajectory of cortical inhibition loss and its underlying mechanisms are not known. Using paired-pulse transcranial magnetic stimulation (ppTMS) and immunohistochemistry, we tracked functional and cellular changes of cortical inhibitory network elements after fluid-percussion injury (FPI) in rats...
November 30, 2016: Cerebral Cortex
https://www.readbyqxmd.com/read/27905510/remarkable-alterations-of-nav1-6-in-reactive-astrogliosis-during-epileptogenesis
#8
Hongyan Zhu, Yuxiao Zhao, Hao Wu, Nan Jiang, Ziyi Wang, Weide Lin, Jiahui Jin, Yonghua Ji
Voltage-gated sodium channels (VGSCs) play a vital role in controlling neuronal excitability. Nav1.6 is the most abundantly expressed VGSCs subtype in the adult central nervous system and has been found to contribute to facilitate the hyperexcitability of neurons after electrical induction of status epilepticus (SE). To clarify the exact expression patterns of Nav1.6 during epileptogenesis, we examined the expression of Nav1.6 at protein and mRNA levels in two distinct animal models of temporal lobe epilepsy (TLE) including a post-SE model induced by kainic acid (KA) intrahippocampal injection and a kindling model evoked by pentylenetetrazole (PTZ)...
December 1, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27896315/altered-oscillatory-dynamics-of-ca1-parvalbumin-basket-cells-during-theta-gamma-rhythmopathies-of-temporal-lobe-epilepsy
#9
Diego Lopez-Pigozzi, François Laurent, Jorge R Brotons-Mas, Mario Valderrama, Manuel Valero, Ivan Fernandez-Lamo, Elena Cid, Daniel Gomez-Dominguez, Beatriz Gal, Liset Menendez de la Prida
Recent reports in human demonstrate a role of theta-gamma coupling in memory for spatial episodes and a lack of coupling in people experiencing temporal lobe epilepsy, but the mechanisms are unknown. Using multisite silicon probe recordings of epileptic rats engaged in episodic-like object recognition tasks, we sought to evaluate the role of theta-gamma coupling in the absence of epileptiform activities. Our data reveal a specific association between theta-gamma (30-60 Hz) coupling at the proximal stratum radiatum of CA1 and spatial memory deficits...
November 2016: ENeuro
https://www.readbyqxmd.com/read/27889489/the-drug-candidate-adx71441-is-a-novel-potent-and-selective-positive-allosteric-modulator-of-the-gabab-receptor-with-a-potential-for-treatment-of-anxiety-pain-and-spasticity
#10
Mikhail Kalinichev, Françoise Girard, Hasnaà Haddouk, Mélanie Rouillier, Eric Riguet, Isabelle Royer-Urios, Vincent Mutel, Robert Lütjens, Sonia Poli
Positive allosteric modulation of the GABAB receptor is a promising alternative to direct activation of the receptor as a therapeutic approach for treatment of addiction, chronic pain, anxiety, epilepsy, autism, Fragile X syndrome, and psychosis. Here we describe in vitro and in vivo characterization of a novel, potent and selective GABAB positive allosteric modulator (PAM) N-(5-(4-(4-chloro-3-fluorobenzyl)-6-methoxy-3,5-dioxo-4,5-dihydro-1,2,4-triazin-2(3H)-yl)-2-fluorophenyl)acetamide (ADX71441). In vitro, Schild plot and reversibility tests at the target confirmed PAM properties of the compound...
November 23, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27881950/a-new-approach-of-modified-submerged-patch-clamp-recording-reveals-interneuronal-dynamics-during-epileptiform-oscillations
#11
Gareth Morris, Premysl Jiruska, John G R Jefferys, Andrew D Powell
Highlights Simultaneous epileptiform LFPs and single-cell activity can be recorded in the membrane chamber.Interneuron firing can be linked to epileptiform high frequency activity.Fast ripples, unique to chronic epilepsy, can be modeled in ex vivo tissue from TeNT-treated rats. Traditionally, visually-guided patch clamp in brain slices using submerged recording conditions has been required to characterize the activity of individual neurons. However, due to limited oxygen availability, submerged conditions truncate fast network oscillations including epileptiform activity...
2016: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/27880801/ampa-receptor-antagonist-nbqx-decreased-seizures-by-normalization-of-perineuronal-nets
#12
Wen Chen, Yan-Shuang Li, Jing Gao, Xiao-Ying Lin, Xiao-Hong Li
Epilepsy is a serious brain disorder with diverse seizure types and epileptic syndromes. AMPA receptor antagonist 2,3-dihydroxy-6-nitro-7-sulfamoyl-benzoquinoxaline-2,3-dione (NBQX) attenuates spontaneous recurrent seizures in rats. However, the anti-epileptic effect of NBQX in chronic epilepsy model is poorly understood. Perineuronal nets (PNNs), specialized extracellular matrix structures, surround parvalbumin-positive inhibitory interneurons, and play a critical role in neuronal cell development and synaptic plasticity...
2016: PloS One
https://www.readbyqxmd.com/read/27873133/altered-expression-of-cxcl13-and-cxcr5-in-intractable-temporal-lobe-epilepsy-patients-and-pilocarpine-induced-epileptic-rats
#13
Ruohan Li, Limin Ma, Hao Huang, Shu Ou, Jinxian Yuan, Tao Xu, Xinyuan Yu, Xi Liu, Juan Yang, Yangmei Chen, Xi Peng
The mechanisms that underlie the pathogenesis of epilepsy are still unclear. Recent studies have indicated that inflammatory processes occurring in the brain are involved in a common and crucial mechanism in epileptogenesis. C-X-C motif chemokine ligand 13 (CXCL13) and its only receptor, C-X-C motif chemokine receptor 5 (CXCR5), are highly expressed in the central nervous system (CNS) and participate in inflammatory responses. The present study aimed to assess the expression of CXCL13 and CXCR5 in the brain tissues of both patients with intractable epilepsy (IE) and a rat model (lithium-pilocarpine) of temporal lobe epilepsy (TLE) to identify possible roles of the CXCL13-CXCR5 signaling pathway in epileptogenesis...
November 21, 2016: Neurochemical Research
https://www.readbyqxmd.com/read/27872690/the-effects-of-kainic-acid-induced-seizure-on-gene-expression-of-brain-neurotransmitter-receptors-in-mice-using-rt-2-pcr-array
#14
Taghi Naserpour Farivar, Marjan Nassiri-Asl, Pouran Johari, Reza Najafipour, Farid Hajiali
INTRODUCTION: Kainic acid (KA) induces neuropathological changes in specific regions of the mouse hippocampus comparable to changes seen in patients with chronic temporal lobe epilepsy (TLE). According to different studies, the expression of a number of genes are altered in the adult rat hippocampus after status epilepticus (SE) induced by KA. This study aimed to quantitatively evaluate changes in the gene expression of brain neurotransmitter receptors one week after administration of kainic acid in the mouse hippocampus...
October 2016: Basic and Clinical Neuroscience
https://www.readbyqxmd.com/read/27866083/neuroanatomical-differences-in-fast-and-slow-rat-strains-with-differential-vulnerability-to-kindling-and-behavioral-comorbidities
#15
Pragati Sharma, Stefanie Dedeurwaerdere, Michael A D Vandenberg, Ke Fang, Leigh A Johnston, Sandy R Shultz, Terence J O'Brien, Krista L Gilby
OBJECTIVE: The neurobiological factors underlying a predisposition towards developing epilepsy and its common behavioral comorbidities are poorly understood. FAST rats are a strain that has been selectively bred for enhanced vulnerability to kindling, while the SLOW strain has been bred to be resistant to kindling. FAST rats also exhibit behavioral traits reminiscent of those observed in neurodevelopmental disorders (autism spectrum disorder (ASD)/attention-deficit/hyperactivity disorder (ADHD)) commonly comorbid with epilepsy...
November 17, 2016: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/27865173/accelerated-cognitive-decline-in-a-rodent-model-for-temporal-lobe-epilepsy
#16
Sandra Schipper, Marlien W Aalbers, Kim Rijkers, Melanie Lagiere, Jan G Bogaarts, Arjan Blokland, Sylvia Klinkenberg, Govert Hoogland, Johan S H Vles
OBJECTIVE: Cognitive impairment is frequently observed in patients with temporal lobe epilepsy. It is hypothesized that cumulative seizure exposure causes accelerated cognitive decline in patients with epilepsy. We investigated the influence of seizure frequency on cognitive decline in a rodent model for temporal lobe epilepsy. METHODS: Neurobehavioral assessment was performed before and after surgery, after the induction of self-sustaining limbic status epilepticus (SSLSE), and in the chronic phase in which rats experienced recurrent seizures...
November 16, 2016: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/27864845/activity-of-the-anticonvulsant-lacosamide-in-experimental-and-human-epilepsy-via-selective-effects-on-slow-na-channel-inactivation
#17
Dominik Holtkamp, Thoralf Opitz, Isabelle Niespodziany, Christian Wolff, Heinz Beck
OBJECTIVE: In human epilepsy, pharmacoresistance to antiepileptic drug therapy is a major problem affecting ~30% of patients with epilepsy. Many classical antiepileptic drugs target voltage-gated sodium channels, and their potent activity in inhibiting high-frequency firing has been attributed to their strong use-dependent blocking action. In chronic epilepsy, a loss of use-dependent block has emerged as a potential cellular mechanism of pharmacoresistance for anticonvulsants acting on voltage-gated sodium channels...
November 19, 2016: Epilepsia
https://www.readbyqxmd.com/read/27853355/anticonvulsant-effects-of-isomeric-nonimidazole-histamine-h3-receptor-antagonists
#18
Bassem Sadek, Ali Saad, Johannes Stephan Schwed, Lilia Weizel, Miriam Walter, Holger Stark
Phenytoin (PHT), valproic acid, and modern antiepileptic drugs (AEDs), eg, remacemide, loreclezole, and safinamide, are only effective within a maximum of 70%-80% of epileptic patients, and in many cases the clinical use of AEDs is restricted by their side effects. Therefore, a continuous need remains to discover innovative chemical entities for the development of active and safer AEDs. Ligands targeting central histamine H3 receptors (H3Rs) for epilepsy might be a promising therapeutic approach. To determine the potential of H3Rs ligands as new AEDs, we recently reported that no anticonvulsant effects were observed for the (S)-2-(4-(3-(piperidin-1-yl)propoxy)benzylamino)propanamide (1)...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27852797/modulation-of-mir-146a-complement-factor-h-mediated-inflammatory-responses-in-a-rat-model-of-temporal-lobe-epilepsy
#19
Fang He, Bei Liu, Qiang Meng, Yang Sun, Weiwen Wang, Chao Wang
Increasing evidence supports the involvement of inflammatory and immune processes in temporal lobe epilepsy (TLE). MicroRNAs (miRNA) represent small regulatory RNA molecules that have been shown to act as negative regulators of gene expression controlling different biological processes, including immune-system homeostasis and function. We investigated the expression and cellular distribution of miRNA-146a (miR-146a) in a rat model of TLE. Prominent upregulation of miR-146a activation was evident at 1 week after status epilepticus (SE) and persisted in the chronic phase...
November 16, 2016: Bioscience Reports
https://www.readbyqxmd.com/read/27847128/effective-g-protein-coupling-of-y2-receptors-along-axonal-fiber-tracts-and-its-relevance-for-epilepsy
#20
Elisabeth Dum, Sabine Fürtinger, Elisabeth Gasser, Anneliese Bukovac, Meinrad Drexel, Ramon Tasan, Günther Sperk
Neuropeptide Y (NPY)-Y2 receptors are G-protein coupled receptors and, upon activation, induce opening of potassium channels or closing of calcium channels. They are generally presynaptically located. Depending on the neuron in which they are expressed they mediate inhibition of release of NPY and of the neuron's classical transmitter GABA, glutamate or noradrenaline, respectively. Here we provide evidence that Y2 receptor binding is inhibited dose-dependently by GTPγS along Schaffer collaterals, the stria terminalis and the fimbria indicating that Y2 receptors are functionally coupled to G-proteins along these fiber tracts...
October 26, 2016: Neuropeptides
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