Results 211 to 220 of about 49,773 (253)
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Sodium channel blockers are effective for benign infantile epilepsy
Seizure, 2021To examine the efficacy and tolerance of the antiseizure medications lacosamide (LCM) and levetiracetam (LEV) in patients with benign infantile epilepsy (BIE).The clinical data of 24 children with BIE seen between 2014 and 2020 were collected retrospectively, and treatment, effectiveness, and adverse effects were examined.
Shingo, Numoto +5 more
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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 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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Molecular design of new sodium channel blockers
Biochemical and Biophysical Research Communications, 2011Animal toxins targeting voltage-gated sodium channels (VGSCs) have been considered as valuable tools for studying pharmacological functions of VGSCs. Recently we have reported that Drosotoxin (DrTx), an evolution-guided chimeric peptide, exhibits highly selective blocking activity to tetrodotoxin-resistant (TTX-R) Na(+) channels in rat dorsal root ...
Ping, Li, Shunyi, Zhu
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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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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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Voltage-Gated Sodium Channel Blockers as Immunomodulators
Recent Patents on CNS Drug Discovery, 2006Several Voltage-Gated Sodium Channels (VGSC) are widely expressed on lymphocytes and macrophages but their role in immune function is still debated. Nevertheless, Na(+) influx through VGSC is required for lymphocytes activation and proliferation, since these responses are blocked by Na(+)-free medium or by VGSC blockers.
ROSELLI F +2 more
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Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers
Journal of Medicinal Chemistry, 1994The synthesis and structure-activity relationships of a series of phenylacetamides related to N-[3-(2,6-dimethyl-1-piperidinyl)propyl]-alpha-phenylbenzeneacetamide (1) (PD85639) acting at the voltage-dependent Na+ channel are described. All structural variations for this study were made in the phenylacetic acid portion of these molecules, and the ...
I, Roufos +5 more
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Sodium channel blockers: a patent review (2010 – 2014)
Expert Opinion on Therapeutic Patents, 2014Abnormal activity of voltage-gated sodium channels (VGSCs) is related to several pathological processes, including cardiac arrhythmias, epilepsy, cancer, neurodegenerative diseases, spasticity, chronic and neuropathic pain. As such VGSCs are considered important therapeutic targets.This review summarized > 30 patents on sodium channel blockers, having ...
ZULIANI, Valentina +3 more
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N-Aryl azacycles as novel sodium channel blockers
Bioorganic & Medicinal Chemistry Letters, 2015We have identified a new series of N-aryl azacycles as sodium channel blockers, which showed good potency on Nav1.7 in FLIPR-based and electrophysiological functional assays. Analogs from this series possessed selectivity over hERG, reasonable oral exposure in rat PK studies and are predicted to have limited CNS penetration.
Stephen M, Lynch +6 more
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