Search Results - "Krafte, Douglas"
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Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels
Published in Proceedings of the National Academy of Sciences - PNAS (16-07-2013)“…Voltage-gated sodium (Na ᵥ) channels play a fundamental role in the generation and propagation of electrical impulses in excitable cells. Here we describe two…”
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A comprehensive approach to identifying repurposed drugs to treat SCN8A epilepsy
Published in Epilepsia (Copenhagen) (01-04-2018)“…Summary Objective Many previous studies of drug repurposing have relied on literature review followed by evaluation of a limited number of candidate compounds…”
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A-887826 is a structurally novel, potent and voltage-dependent Na(v)1.8 sodium channel blocker that attenuates neuropathic tactile allodynia in rats
Published in Neuropharmacology (01-09-2010)“…Activation of sodium channels is essential to action potential generation and propagation. Recent genetic and pharmacological evidence indicates that…”
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A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat
Published in Proceedings of the National Academy of Sciences - PNAS (15-05-2007)“…Activation of tetrodotoxin-resistant sodium channels contributes to action potential electrogenesis in neurons. Antisense oligonucleotide studies directed…”
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Sodium channels and nociception: recent concepts and therapeutic opportunities
Published in Current opinion in pharmacology (01-02-2008)“…Recent scientific advances have enhanced our understanding of the role voltage-gated sodium channels play in pain sensation. Human data on Nav1.7 show that…”
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Discovery and Biological Evaluation of 5-Aryl-2-furfuramides, Potent and Selective Blockers of the Nav1.8 Sodium Channel with Efficacy in Models of Neuropathic and Inflammatory Pain
Published in Journal of medicinal chemistry (14-02-2008)“…Nav1.8 (also known as PN3) is a tetrodotoxin-resistant (TTx-r) voltage-gated sodium channel (VGSC) that is highly expressed on small diameter sensory neurons…”
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Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain
Published in Bioorganic & medicinal chemistry (15-11-2010)“…Na(v)1.8 (also known as PN3) is a tetrodotoxin-resistant (TTx-r) voltage-gated sodium channel (VGSC) that is highly expressed on small diameter sensory…”
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Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives
Published in Bioorganic & medicinal chemistry letters (15-11-2010)“…A series of aryl-substituted nicotinamide derivatives with selective inhibitory activity against the Na(v)1.8 sodium channel is reported. Replacement of the…”
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The Effect of κ-Opioid Receptor Agonists on Tetrodotoxin-Resistant Sodium Channels in Primary Sensory Neurons
Published in Anesthesia and analgesia (01-08-2009)“…A non-opioid receptor-mediated inhibition of sodium channels in dorsal root ganglia (DRGs) by kappa-opioid receptor agonists (kappa-ORAs) has been reported to…”
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Ion channels: applications in ion channel drug discovery
Published in Combinatorial chemistry & high throughput screening (01-01-2009)Get more information
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Subtype-selective Nav1.8 sodium channel blockers: Identification of potent, orally active nicotinamide derivatives
Published in Bioorganic & medicinal chemistry letters (15-11-2010)“…A series of aryl-substituted nicotinamide derivatives with selective inhibitory activity against the Nav1.8 sodium channel is reported. Replacement of the…”
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Tenidap, a novel anti-inflammatory agent, is an opener of the inwardly rectifying K + channel hKir2.3
Published in European journal of pharmacology (25-01-2002)“…We studied the effect of a novel anti-inflammatory agent, tenidap, on a cloned inwardly rectifying K + channel, hKir2.3. Tenidap (a) potently potentiated 86Rb…”
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Prevention of Proteinuria by a Novel, Subnanomolar ApoL1 Inhibitor: FR-OR105
Published in Journal of the American Society of Nephrology (01-11-2023)Get full text
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Block of Nav1.8 by Small Molecules
Published in Channels (Austin, Tex.) (01-05-2007)“…Sodium channels are key proteins in regulating neuronal excitability and accumulating data suggest that specific subtypes of voltage-dependent sodium channels…”
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Decrease of inward rectification as a mechanism for arachidonic acid-induced potentiation of hKir2.3
Published in European biophysics journal (01-12-2002)“…Previously, we showed that arachidonic acid (AA) potentiates currents flowing through a cloned human inwardly rectifying K(+) channel, hKir2.3. The mechanism…”
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Synthesis and Structure-Activity Relationships of 6-Heterocyclic-Substituted Purines as Inactivation Modifiers of Cardiac Sodium Channels
Published in Journal of medicinal chemistry (01-07-1995)“…Purine-based analogs of SDZ 211-500 (5) were prepared and evaluated as inactivation modifiers of guinea pig or human cardiac sodium (Na) channels expressed in…”
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Direct activation of an inwardly rectifying potassium channel by arachidonic acid
Published in Molecular pharmacology (01-05-2001)“…Arachidonic acid (AA) is an important constituent of membrane phospholipids and can be liberated by activation of cellular phospholipases. AA modulates a…”
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A comprehensive approach to identifying repurposed drugs to treat SCN 8A epilepsy
Published in Epilepsia (Copenhagen) (01-04-2018)“…Summary Objective Many previous studies of drug repurposing have relied on literature review followed by evaluation of a limited number of candidate compounds…”
Get full text
Journal Article