Advances in Design and Development of Sodium Channel Blockers

Zuliani, Valentina; Amori, Laura; Rivara, Mirko

doi:10.1007/978-3-642-19922-6_4

Ion Channels and Their Inhibitors 2011

DOI: 10.1007/978-3-642-19922-6_4

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Advances in Design and Development of Sodium Channel Blockers

Valentina Zuliani

Laura Amori²,

Mirko Rivara³

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Cited by 2 publications

References 222 publications

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Advances in Targeting Voltage‐Gated Sodium Channels with Small Molecules

Nardi¹,

Damann²,

Hertrampf³

et al. 2012

ChemMedChem

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Blockade of voltage-gated sodium channels (VGSCs) has been used successfully in the clinic to enable control of pathological firing patterns that occur in conditions as diverse as chronic pain, epilepsy, and arrhythmias. Herein we review the state of the art in marketed sodium channel inhibitors, including a brief compendium of their binding sites and of the cellular and molecular biology of sodium channels. Despite the preferential action of this drug class toward over-excited cells, which significantly limits potential undesired side effects on other cells, the need to develop a second generation of sodium channel inhibitors to overcome their critical clinical shortcomings is apparent. Current approaches in drug discovery to deliver novel and truly innovative sodium channel inhibitors is next presented by surveying the most recent medicinal chemistry breakthroughs in the field of small molecules and developments in automated patch-clamp platforms. Various strategies aimed at identifying small molecules that target either particular isoforms of sodium channels involved in specific diseases or anomalous sodium channel currents, irrespective of the isoform by which they have been generated, are critically discussed and revised.

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Advances in Targeting Voltage‐Gated Sodium Channels with Small Molecules

Nardi¹,

Damann²,

Hertrampf³

et al. 2012

ChemMedChem

View full text Add to dashboard Cite

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Fusion of laser-induced breakdown spectroscopy technology and deep learning: a new method to identify malignant and benign lung tumors with high accuracy

Lin,

Li,

Lin

et al. 2023

Anal Bioanal Chem

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Advances in Design and Development of Sodium Channel Blockers

Cited by 2 publications

References 222 publications

Advances in Targeting Voltage‐Gated Sodium Channels with Small Molecules

Advances in Targeting Voltage‐Gated Sodium Channels with Small Molecules

Fusion of laser-induced breakdown spectroscopy technology and deep learning: a new method to identify malignant and benign lung tumors with high accuracy

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