Search Results - "Goodchild, Samuel J"
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1
Cannabidiol increases gramicidin current in human embryonic kidney cells: An observational study
Published in PloS one (01-08-2022)“…Gramicidin is a monomeric protein that is thought to non-selectively conduct cationic currents and water. Linear gramicidin is considered an antibiotic. This…”
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2
Sequence of Gating Charge Movement and Pore Gating in hERG Activation and Deactivation Pathways
Published in Biophysical journal (24-03-2015)“…KV11.1 voltage-gated K+ channels are noted for unusually slow activation, fast inactivation, and slow deactivation kinetics, which tune channel activity to…”
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3
Selective NaV1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain
Published in Cell reports (Cambridge) (18-09-2018)“…Selective block of NaV1.7 promises to produce non-narcotic analgesic activity without motor or cognitive impairment. Several NaV1.7-selective blockers have…”
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4
Local anesthetic inhibition of a bacterial sodium channel
Published in The Journal of general physiology (01-06-2012)“…Recent structural breakthroughs with the voltage-gated sodium channel from Arcobacter butzleri suggest that such bacterial channels may provide a structural…”
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5
Non-psychotropic phytocannabinoid interactions with voltage-gated sodium channels: An update on cannabidiol and cannabigerol
Published in Frontiers in physiology (10-11-2022)“…Phytocannabinoids, found in the plant, , are an important class of natural compounds with physiological effects. These compounds can be generally divided into…”
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6
Pharmacological determination of the fractional block of Nav channels required to impair neuronal excitability and ex vivo seizures
Published in Frontiers in cellular neuroscience (29-09-2022)“…Voltage-gated sodium channels (Nav) are essential for the initiation and propagation of action potentials in neurons. Of the nine human channel subtypes,…”
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7
Expanding the genotype-phenotype spectrum in SCN8A-related disorders
Published in BMC neurology (17-01-2024)“…SCN8A-related disorders are a group of variable conditions caused by pathogenic variations in SCN8A. Online Mendelian Inheritance in Man (OMIM) terms them as…”
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8
Allosteric Block of KCa2 Channels by Apamin
Published in The Journal of biological chemistry (27-08-2010)“…Activation of small conductance calcium-activated potassium (KCa2) channels can regulate neuronal firing and synaptic plasticity. They are characterized by…”
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9
Blockade of Permeation by Potassium but Normal Gating of the G628S Nonconducting hERG Channel Mutant
Published in Biophysical journal (03-08-2011)“…G628S is a mutation in the signature sequence that forms the selectivity filter of the human ether-a-go-go-related gene (hERG) channel (GFG) and is associated…”
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10
Inhibitory effects of cannabidiol on voltage-dependent sodium currents
Published in The Journal of biological chemistry (26-10-2018)“…Cannabis sativa contains many related compounds known as phytocannabinoids. The main psychoactive and nonpsychoactive compounds are Δ9-tetrahydrocannabinol…”
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11
Molecular and functional determinants of local anesthetic inhibition of NaChBac
Published in Channels (Austin, Tex.) (01-09-2012)“…In our recent publication, we describe the local anesthetic (LA) inhibition of the prokaryotic voltage gated sodium channel NaChBac. Despite the numerous…”
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12
Cannabidiol inhibits the skeletal muscle Nav1.4 by blocking its pore and by altering membrane elasticity
Published in The Journal of general physiology (03-05-2021)“…Cannabidiol (CBD) is the primary nonpsychotropic phytocannabinoid found in Cannabis sativa, which has been proposed to be therapeutic against many conditions,…”
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13
The contribution of Na V 1.6 to the efficacy of voltage-gated sodium channel inhibitors in wild type and Na V 1.6 gain-of-function (GOF) mouse seizure control
Published in British journal of pharmacology (01-10-2024)“…Inhibitors of voltage-gated sodium channels (Na s) are important anti-epileptic drugs, but the contribution of specific channel isoforms is unknown since…”
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14
The contribution of NaV1.6 to the efficacy of voltage‐gated sodium channel inhibitors in wild type and NaV1.6 gain‐of‐function (GOF) mouse seizure control
Published in British journal of pharmacology (01-10-2024)“…Background and Purpose Inhibitors of voltage‐gated sodium channels (NaVs) are important anti‐epileptic drugs, but the contribution of specific channel isoforms…”
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15
Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective NaV1.6 Inhibitors with Efficacy in Mouse Models of Epilepsy
Published in Journal of medicinal chemistry (14-11-2019)“…Nonselective antagonists of voltage-gated sodium (NaV) channels have been long used for the treatment of epilepsies. The efficacy of these drugs is thought to…”
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16
Molecular Pharmacology of Selective NaV1.6 and Dual NaV1.6/NaV1.2 Channel Inhibitors that Suppress Excitatory Neuronal Activity Ex Vivo
Published in ACS chemical neuroscience (20-03-2024)“…Voltage-gated sodium channel (NaV) inhibitors are used to treat neurological disorders of hyperexcitability such as epilepsy. These drugs act by attenuating…”
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17
Small conductance calcium-activated potassium channels: from structure to function
Published in Progress in neurobiology (01-07-2010)“…The cloning of K(Ca)2 channels revealed three subtypes, with each displaying distinct but partially overlapping expression distributions in the mammalian CNS…”
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18
Identification of aryl sulfonamides as novel and potent inhibitors of NaV1.5
Published in Bioorganic & medicinal chemistry letters (01-08-2021)“…[Display omitted] •A series of novel aryl sulfonamide NaV1.5 inhibitors were described.•Compound (-)-6 is a potent NaV1.5 inhibitor with high selectivity over…”
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NBI-921352, a first-in-class, NaV1.6 selective, sodium channel inhibitor that prevents seizures in Scn8a gain-of-function mice, and wild-type mice and rats
Published in eLife (02-03-2022)“…NBI-921352 (formerly XEN901) is a novel sodium channel inhibitor designed to specifically target Na V 1.6 channels. Such a molecule provides a…”
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Molecular Pharmacology of Selective Na V 1.6 and Dual Na V 1.6/Na V 1.2 Channel Inhibitors that Suppress Excitatory Neuronal Activity Ex Vivo
Published in ACS chemical neuroscience (20-03-2024)“…Voltage-gated sodium channel (Na ) inhibitors are used to treat neurological disorders of hyperexcitability such as epilepsy. These drugs act by attenuating…”
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