Search Results - "Kaminski, Rafal M."
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Repurposed molecules for antiepileptogenesis: Missing an opportunity to prevent epilepsy?
Published in Epilepsia (Copenhagen) (01-03-2020)“…Prevention of epilepsy is a great unmet need. Acute central nervous system (CNS) insults such as traumatic brain injury (TBI), cerebrovascular accidents (CVA),…”
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Neuroinflammatory targets and treatments for epilepsy validated in experimental models
Published in Epilepsia (Copenhagen) (01-07-2017)“…Summary A large body of evidence that has accumulated over the past decade strongly supports the role of inflammation in the pathophysiology of human epilepsy…”
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Brivaracetam: Rationale for discovery and preclinical profile of a selective SV2A ligand for epilepsy treatment
Published in Epilepsia (Copenhagen) (01-04-2016)“…Summary Despite availability of effective antiepileptic drugs (AEDs), many patients with epilepsy continue to experience refractory seizures and adverse…”
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Nrf2 defense pathway: Experimental evidence for its protective role in epilepsy
Published in Annals of neurology (01-10-2013)“…Objective Epigenetic mechanisms involved in transcriptional regulation of multiple molecular pathways are potentially attractive therapeutic interventions for…”
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Rapid epileptogenesis in the mouse pilocarpine model: Video-EEG, pharmacokinetic and histopathological characterization
Published in Experimental neurology (01-12-2012)“…Temporal lobe epilepsy (TLE) is the most common form of drug-resistant epilepsy and several rodent models allow studying the pathophysiology of this disorder…”
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n-3 Docosapentaenoic acid-derived protectin D1 promotes resolution of neuroinflammation and arrests epileptogenesis
Published in Brain (London, England : 1878) (01-11-2018)“…Frigerio et al. report that pro-resolving mechanisms of neuroinflammation are dysregulated during epileptogenesis, thereby promoting a persistent…”
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Discovery of (R)‑N‑Benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide [(R)-AS‑1], a Novel Orally Bioavailable EAAT2 Modulator with Drug-like Properties and Potent Antiseizure Activity In Vivo
Published in Journal of medicinal chemistry (08-09-2022)“…( R )-7 [( R )-AS-1] showed broad-spectrum antiseizure activity across in vivo mouse seizure models: maximal electroshock (MES), 6 Hz (32/44 mA), acute…”
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TRPV1 channel in the pathophysiology of epilepsy and its potential as a molecular target for the development of new antiseizure drug candidates
Published in Progress in neurobiology (01-09-2024)“…Identification of transient receptor potential cation channel, subfamily V member 1 (TRPV1), also known as capsaicin receptor, in 1997 was a milestone…”
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The Search for New Anticonvulsants in a Group of (2,5-Dioxopyrrolidin-1-yl)(phenyl)Acetamides with Hybrid Structure-Synthesis and In Vivo/In Vitro Studies
Published in International journal of molecular sciences (20-11-2020)“…Epilepsy belongs to the most common and debilitating neurological disorders with multifactorial pathophysiology and a high level of drug resistance. Therefore,…”
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KA‐104, a new multitargeted anticonvulsant with potent antinociceptive activity in preclinical models
Published in Epilepsia (Copenhagen) (01-10-2020)“…Objective The main objective of the present work was to assess the utility of KA‐104 as potential therapy for drug‐resistant seizures and neuropathic pain, and…”
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A systems-level framework for drug discovery identifies Csf1R as an anti-epileptic drug target
Published in Nature communications (03-09-2018)“…The identification of drug targets is highly challenging, particularly for diseases of the brain. To address this problem, we developed and experimentally…”
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Identification of New Compounds with Anticonvulsant and Antinociceptive Properties in a Group of 3-substituted (2,5-dioxo-pyrrolidin-1-yl)(phenyl)-Acetamides
Published in International journal of molecular sciences (03-12-2021)“…We report herein a series of water-soluble analogues of previously described anticonvulsants and their detailed in vivo and in vitro characterization. The…”
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Novel Alaninamide Derivatives with Drug-like Potential for Development as Antiseizure and Antinociceptive TherapiesIn Vitro and In Vivo Characterization
Published in ACS chemical neuroscience (05-06-2024)“…In the present study, a series of original alaninamide derivatives have been designed applying a combinatorial chemistry approach, synthesized, and…”
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Inhibition of CHIT1 as a novel therapeutic approach in idiopathic pulmonary fibrosis
Published in European journal of pharmacology (15-03-2022)“…Idiopathic pulmonary fibrosis (IPF) is a progressive and eventually fatal lung disease with a complex etiology. Approved drugs, nintedanib and pirfenidone,…”
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Discovery and Profiling of New Multimodal Phenylglycinamide Derivatives as Potent Antiseizure and Antinociceptive Drug Candidates
Published in ACS chemical neuroscience (04-09-2024)“…We developed a focused series of original phenyl-glycinamide derivatives which showed potent activity across in vivo mouse seizure models, namely, maximal…”
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Inhibiting Epileptiform Activity in Cognitive Disorders: Possibilities for a Novel Therapeutic Approach
Published in Frontiers in neuroscience (15-10-2020)“…Cognitive impairment is a common and seriously debilitating symptom of various mental and neurological disorders including autism, attention deficit…”
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Inhibition of glutamate decarboxylase (GAD) by ethyl ketopentenoate (EKP) induces treatment-resistant epileptic seizures in zebrafish
Published in Scientific reports (03-08-2017)“…Epilepsy is a chronic brain disorder characterized by recurrent seizures due to abnormal, excessive and synchronous neuronal activities in the brain. It…”
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Asymmetric synthesis and in vivo/in vitro characterization of new hybrid anticonvulsants derived from (2,5-dioxopyrrolidin-1-yl)phenylacetamides
Published in Bioorganic chemistry (01-04-2021)“…[Display omitted] •New hybrid anticonvulsants were obtained applying the multistep asymmetric procedure.•X-ray crystallography was used to solve the spatial…”
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Role of GluK1 kainate receptors in seizures, epileptic discharges, and epileptogenesis
Published in The Journal of neuroscience (23-04-2014)“…Kainate receptors containing the GluK1 subunit have an impact on excitatory and inhibitory neurotransmission in brain regions, such as the amygdala and…”
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Anticonvulsant and antiepileptogenic effects of system xc− inactivation in chronic epilepsy models
Published in Epilepsia (Copenhagen) (01-07-2019)“…Objective The cystine/glutamate antiporter system xc− could represent a new target for antiepileptogenic treatments due to its crucial roles in glutamate…”
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