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benzothiazole/accidente cerebrovascular
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The stroke pharmacopeia: promising experimental therapies.
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The development of promising acute stroke treatments is the fruit of the growing appreciation for the complex biochemical processes within neuronal tissue that commence immediately after the onset of ischemia. These biochemical cascades can be modified either by direct pharmacologic mitigation or by
Lubeluzole for acute ischaemic stroke.
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BACKGROUND
Experimental studies have shown that ischaemic insults cause excess release of excitatory amino acid (EAA) neurotransmitters, particularly glutamate. Glutamate re-uptake is impaired under ischaemic conditions. In preclinical models of stroke, antagonists of excitatory amino acids or of
Lubeluzole treatment of acute ischemic stroke. The US and Canadian Lubeluzole Ischemic Stroke Study Group.
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OBJECTIVE
Lubeluzole is a novel benzothiazole compound that has shown neuroprotective activity in preclinical models of ischemic stroke. The present multicenter, double-blind, placebo-controlled study was conducted to assess the efficacy and safety of lubeluzole in the treatment of ischemic
Multinational randomised controlled trial of lubeluzole in acute ischaemic stroke. European and Australian Lubeluzole Ischaemic Stroke Study Group.
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OBJECTIVE
Lubeluzole is a benzothiazole derivative that has shown neuroprotective properties in different experimental models. This multicentre, double-blind, placebo-controlled trial was conducted to assess the safety and efficacy of lubeluzole in patients with an acute ischaemic
Lubeluzole protects sensorimotor function and reduces infarct size in a photochemical stroke model in rats.
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Posttreatment with lubeluzole, the S-isomer of a novel 3,4-difluoro benzothiazole, potently rescued tactile/proprioceptive hindlimb placing reactions contralateral to unilateral thrombotic infarcts in the hindlimb area of the parietal sensorimotor neocortex of rats. Administered at 5 min
Differential effects of the neuroprotectant lubeluzole on bovine and mouse chromaffin cell calcium channel subtypes.
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1. The effects of lubeluzole (a neuroprotective benzothiazole derivative) and its (-) enantiomer R91154 on whole-cell currents through Ca2+ channels, with 10 mM Ba2+ as charge carrier (IBa), have been studied in bovine and mouse voltage-clamped adrenal chromaffin cells. Currents generated by
Molecular Insights into hERG Potassium Channel Blockade by Lubeluzole.
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OBJECTIVE
Lubeluzole is a benzothiazole derivative that has shown neuroprotective properties in preclinical models of ischemic stroke. However, clinical research on lubeluzole is now at a standstill, since lubeluzole seems to be associated with the acquired long QT syndrome and ventricular
Effects of Benzothiazolamines on Voltage-Gated Sodium Channels.
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Benzothiazole is a versatile fused heterocycle that aroused much interest in drug discovery as anticonvulsant, neuroprotective, analgesic, anti-inflammatory, antimicrobial, and anticancer. Two benzothiazolamines, riluzole and lubeluzole, are known blockers of voltage-gated sodium (Nav) channels.
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