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Sodium channel blockers for neuropathic pain [PDF]
The voltage-gated sodium channels (VGSCs) play a fundamental role in controlling cellular excitability and their abnormal activity is related to several pathological processes, including cardiac arrhythmias, epilepsy, neurodegenerative diseases, spasticity, chronic and neuropathic pain. In particular, neuropathic pain (e.g., postherpetic and trigeminal
ZULIANI, Valentina +3 more
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Dibenzazepines and dibenzoxazepines as sodium channel blockers
Bioorganic and Medicinal Chemistry Letters, 2015We have identified two related series of dibenzazepine and dibenzoxazepine sodium channel blockers, which showed good potency on Nav1.7 in FLIPR-based and electrophysiological functional assays.
Laykea Tafesse
exaly +3 more sources
Epilepsy and sodium channel blockers
Expert Opinion on Therapeutic Patents, 2002Epilepsy is one of the most frequent neurological diseases and although most patients nowadays respond well to anti-epileptic drugs (AED), 30 - 40% of them still present seizures despite treatment ...
Daniel Bertrand
exaly +2 more sources
Neuropathic pain: preclinical and early clinical progress with voltage-gated sodium channel blockers [PDF]
Introduction: Neuropathic pain is a chronic condition that significantly affects the quality of life of millions of people globally. Most of the pharmacologic treatments currently in use demonstrate modest efficacy and over half of all patients do not ...
Nebojsa Nick Knežević
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Journal of Medicinal Chemistry, 2007
AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Donald J, Kyle, Victor I, Ilyin
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AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Donald J, Kyle, Victor I, Ilyin
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Constrained analogues of tocainide as potent skeletal muscle sodium channel blockers towards the development of antimyotonic agents [PDF]
1-Benzyl-N-(2,6-dimethylphenyl)piperidine-3-carboxamide and 4-benzyl-N-(2,6-dimethylphenyl)piperazine-2-carboxamide, two conformationally restricted analogues of tocainide, were designed and synthesized as voltage-gated skeletal muscle sodium channel ...
Michela De Bellis +2 more
exaly +2 more sources
Sodium Channel Blockers in Neuropathic Pain
Current Pharmaceutical Design, 2005Subtypes of tetrodotoxin resistant voltage-gated sodium channels are involved in the development of certain types of neuropathic pains. After nerve injury hyperexcitability and spontaneous firing develop at the site of injury and also in the dorsal root ganglion cell bodies.
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Metaflumizone is a novel sodium channel blocker insecticide
Veterinary Parasitology, 2007Metaflumizone is a novel semicarbazone insecticide, derived chemically from the pyrazoline sodium channel blocker insecticides (SCBIs) discovered at Philips-Duphar in the early 1970s, but with greatly improved mammalian safety. This paper describes studies confirming that the insecticidal action of metaflumizone is due to the state-dependent blockage ...
V L, Salgado, J H, Hayashi
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Sodium Channel Blockers in the Treatment of Epilepsy
CNS Drugs, 2017Sodium channel blockers have been the mainstay of the pharmacological management of focal and generalised tonic-clonic seizures for more than 70 years. The focus of this paper will be on phenytoin, carbamazepine, lamotrigine, oxcarbazepine, rufinamide, lacosamide and eslicarbazepine acetate. All these antiepileptic drugs have similar efficacy and share
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Polymorphism of a Novel Sodium Ion Channel Blocker
Journal of Pharmaceutical Sciences, 20032-[[4-(4-Fluorophenoxy)phenyl]-methylene]-hydrazinecarboxamide, a member of the semicarbazone family which has shown potential therapeutic use as anticonvulsants, has been found to exist in two polymorphic forms denoted A and B. In addition to reporting aspects of the physical characterization of both forms, the crystal structure of polymorph A has ...
Eugene Y, Cheung +4 more
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