Ion Channel Blockers

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Qi-xin Chen - One of the best experts on this subject based on the ideXlab platform.

  • Ion Channel Blockers and spinal cord injury
    Journal of Neuroscience Research, 2011
    Co-Authors: Wang-mi Liu, Qi-xin Chen
    Abstract:

    The activatIon of a delayed secondary cascade of unsatisfactory cellular and molecular responses after a primary mechanical insult to the spinal cord causes the progressive degeneratIon of this structure. Disturbance of Ionic homeostasis is part of the secondary injury process and plays an integral role in the early stage of spinal cord injury (SCI). The secondary pathology of SCI is complex and involves disturbance of the homeostasis of K(+) , Na(+) , and Ca(2+) . The effect of Ion Channel Blockers on chronic SCI has also been proved. In this Mini-Review, we provide a comprehensive summary of the effects of Ion Channel Blockers on the natural responses after SCI. CombinatIon therapy is based on the roles of Ions and disturbance of their homeostasis in SCI. The effects of Ion Channel Blockers suggest that they have potential in the treatment of SCI, although the complexity of their effects shows that further knowledge is needed before they can be applied clinically.

  • Ion Channel Blockers and spinal cord injury
    Journal of neuroscience research, 2011
    Co-Authors: Wang-mi Liu, Qi-xin Chen
    Abstract:

    The activatIon of a delayed secondary cascade of unsatisfactory cellular and molecular responses after a primary mechanical insult to the spinal cord causes the progressive degeneratIon of this structure. Disturbance of Ionic homeostasis is part of the secondary injury process and plays an integral role in the early stage of spinal cord injury (SCI). The secondary pathology of SCI is complex and involves disturbance of the homeostasis of K+, Na+, and Ca2+. The effect of Ion Channel Blockers on chronic SCI has also been proved. In this Mini-Review, we provide a comprehensive summary of the effects of Ion Channel Blockers on the natural responses after SCI. CombinatIon therapy is based on the roles of Ions and disturbance of their homeostasis in SCI. The effects of Ion Channel Blockers suggest that they have potential in the treatment of SCI, although the complexity of their effects shows that further knowledge is needed before they can be applied clinically. © 2011 Wiley-Liss, Inc.

Wang-mi Liu - One of the best experts on this subject based on the ideXlab platform.

  • Ion Channel Blockers and spinal cord injury
    Journal of Neuroscience Research, 2011
    Co-Authors: Wang-mi Liu, Qi-xin Chen
    Abstract:

    The activatIon of a delayed secondary cascade of unsatisfactory cellular and molecular responses after a primary mechanical insult to the spinal cord causes the progressive degeneratIon of this structure. Disturbance of Ionic homeostasis is part of the secondary injury process and plays an integral role in the early stage of spinal cord injury (SCI). The secondary pathology of SCI is complex and involves disturbance of the homeostasis of K(+) , Na(+) , and Ca(2+) . The effect of Ion Channel Blockers on chronic SCI has also been proved. In this Mini-Review, we provide a comprehensive summary of the effects of Ion Channel Blockers on the natural responses after SCI. CombinatIon therapy is based on the roles of Ions and disturbance of their homeostasis in SCI. The effects of Ion Channel Blockers suggest that they have potential in the treatment of SCI, although the complexity of their effects shows that further knowledge is needed before they can be applied clinically.

  • Ion Channel Blockers and spinal cord injury
    Journal of neuroscience research, 2011
    Co-Authors: Wang-mi Liu, Qi-xin Chen
    Abstract:

    The activatIon of a delayed secondary cascade of unsatisfactory cellular and molecular responses after a primary mechanical insult to the spinal cord causes the progressive degeneratIon of this structure. Disturbance of Ionic homeostasis is part of the secondary injury process and plays an integral role in the early stage of spinal cord injury (SCI). The secondary pathology of SCI is complex and involves disturbance of the homeostasis of K+, Na+, and Ca2+. The effect of Ion Channel Blockers on chronic SCI has also been proved. In this Mini-Review, we provide a comprehensive summary of the effects of Ion Channel Blockers on the natural responses after SCI. CombinatIon therapy is based on the roles of Ions and disturbance of their homeostasis in SCI. The effects of Ion Channel Blockers suggest that they have potential in the treatment of SCI, although the complexity of their effects shows that further knowledge is needed before they can be applied clinically. © 2011 Wiley-Liss, Inc.

Lechoslaw Turski - One of the best experts on this subject based on the ideXlab platform.

  • why did nmda receptor antagonists fail clinical trials for stroke and traumatic brain injury
    Lancet Neurology, 2002
    Co-Authors: Chrysanthy Ikonomidou, Lechoslaw Turski
    Abstract:

    Glutamate N-methyl-D-aspartate (NMDA) receptor antagonists (competitive receptor antagonists, Ion Channel Blockers, and glycine antagonists)—such as selfotel, aptiganel, eliprodil, licostinel and gavestinel—failed to show efficacy in clinical trials of stroke or traumatic brain injury. This failure has been attributed to the deficient properties of the molecules that entered human trials and to inappropriate design of clinical studies. In this article we hypothesise that glutamate may be involved in the acute neurodestructive phase that occurs immediately after traumatic or ischaemic injury (excitotoxicity), but that, after this period, it assumes its normal physiological functIons, which include promotIon of neuronal survival. We propose that NMDA receptor antagonists failed stroke and traumatic brain injury trials in human beings because blockade of synaptic transmissIon mediated by NMDA receptors hinders neuronal survival.

Chrysanthy Ikonomidou - One of the best experts on this subject based on the ideXlab platform.

  • why did nmda receptor antagonists fail clinical trials for stroke and traumatic brain injury
    Lancet Neurology, 2002
    Co-Authors: Chrysanthy Ikonomidou, Lechoslaw Turski
    Abstract:

    Glutamate N-methyl-D-aspartate (NMDA) receptor antagonists (competitive receptor antagonists, Ion Channel Blockers, and glycine antagonists)—such as selfotel, aptiganel, eliprodil, licostinel and gavestinel—failed to show efficacy in clinical trials of stroke or traumatic brain injury. This failure has been attributed to the deficient properties of the molecules that entered human trials and to inappropriate design of clinical studies. In this article we hypothesise that glutamate may be involved in the acute neurodestructive phase that occurs immediately after traumatic or ischaemic injury (excitotoxicity), but that, after this period, it assumes its normal physiological functIons, which include promotIon of neuronal survival. We propose that NMDA receptor antagonists failed stroke and traumatic brain injury trials in human beings because blockade of synaptic transmissIon mediated by NMDA receptors hinders neuronal survival.

Xiaoming Wang - One of the best experts on this subject based on the ideXlab platform.

  • fluorescence based high throughput screening technologies for natural chloride Ion Channel Blockers
    Chemical Research in Toxicology, 2018
    Co-Authors: Yuan Xiao, Yan Liu, Bo Wang, Cong Huo, Xin Jia, Liming Hou, Xiaoming Wang
    Abstract:

    Chloride Channels represent a group of potential drug targets; their Blockers showed significant protecting effect on impaired cells by modulating apoptosis, autophagy, and other cell signals. However, clinical drugs with chloride Channel inhibitory properties have not yet been developed. Natural product extract becomes an underlying candidate satisfied the clinical requirements for its low toxicity, low cost, and abundant sources. Here, a fluorescence-based EYFP-H148Q/I153L-HeLa cell line model was constructed by molecular cloning and verified by real-time polymerase chain reactIon and Western blotting assay. By using this chloride Channel blocker screening model, seven hit compounds chosen from 6988 natural compounds showed the Channel blocking activity. Then the hit compounds were further validated by electrophysiological patch-clamp analysis. Our study preliminarily identified PC-4 as a new chloride Channel inhibitor and demonstrated the reliability and sensitivity of fluorescence-based high throughput screening technologies for discovery of biologically active compounds from natural herbal compounds.

  • Fluorescence-Based High Throughput Screening Technologies for Natural Chloride Ion Channel Blockers
    2018
    Co-Authors: Yuan Xiao, Yan Liu, Bo Wang, Cong Huo, Xin Jia, Liming Hou, Xiaoming Wang
    Abstract:

    Chloride Channels represent a group of potential drug targets; their Blockers showed significant protecting effect on impaired cells by modulating apoptosis, autophagy, and other cell signals. However, clinical drugs with chloride Channel inhibitory properties have not yet been developed. Natural product extract becomes an underlying candidate satisfied the clinical requirements for its low toxicity, low cost, and abundant sources. Here, a fluorescence-based EYFP-H148Q/I153L-HeLa cell line model was constructed by molecular cloning and verified by real-time polymerase chain reactIon and Western blotting assay. By using this chloride Channel blocker screening model, seven hit compounds chosen from 6988 natural compounds showed the Channel blocking activity. Then the hit compounds were further validated by electrophysiological patch-clamp analysis. Our study preliminarily identified PC-4 as a new chloride Channel inhibitor and demonstrated the reliability and sensitivity of fluorescence-based high throughput screening technologies for discovery of biologically active compounds from natural herbal compounds