Inactivation of voltage dependent sodium channels. Medical search. Frequent questions

δ-conotoxin inhibits fast inactivation of voltage-dependent sodium channels. (wikipedia.org)
Here we show that substitution of glutamine for three clustered hydrophobic amino acids, Ile-1488, Phe-1489, and Met-1490, completely removes fast inactivation. (xenbase.org)
The M1476I mutation caused an increased persistent Na⁺ current, a 2- to 3-fold slower fast inactivation, a 6.4 mV depolarizing shift in the midpoint of steady-state inactivation, and an accelerated recovery from fast inactivation compared to the wild-type (WT) channel. (ulaval.ca)
These results indicated that cooling can augment the disruption of the voltage dependence of fast inactivation by M1476I channels. (ulaval.ca)

Sodium channel β1 subunits modulate α subunit gating and cell surface expression and participate in cell adhesive interactions in vitro . (jneurosci.org)
A rat brain Na+ channel alpha subunit with novel gating properties. (xenbase.org)
Primary structure and functional expression of the beta 1 subunit of the rat brain sodium channel. (xenbase.org)
Upregulation of the voltage-gated sodium channel beta2 subunit in neuropathic pain models: characterization of expression in injured and non-injured primary sensory neurons. (springer.com)
It adopts the canonical structural organization of the homo-tetrameric K V superfamily, in which each subunit contains six transmembrane segments (S1-S6), with the first four (S1-S4) forming the voltage-sensing domain (VSD) and the latter two (S5-S6) folding to the pore ( Sun and MacKinnon, 2017 ). (elifesciences.org)
Mutations in four genes have been identified in familial hemiplegic migraine (FHM), from which CACNA1A (FHM type 1) and SCN1A (FHM type 3) code for neuronal voltage-gated calcium or sodium channels, respectively, while ATP1A2 (FHM type 2) encodes the α 2 isoform of the Na + ,K + -ATPase's catalytic subunit, thus classifying FHM primarily as an ion channel/ion transporter pathology. (frontiersin.org)
These effects of [Ca2+]i on delKPQ INaL and inactivation kinetics were not dependent on the presence of the β1 subunit. (biosemiotics2013.org)
Finally, it seems appropriate to consider the "sodium channel syndrome" (mutations in the gene of the α subunit of the sodium channel, SCN5A gene) as a single clinical entity that may manifest in a wide range of phenotypes, to thus have a better insight on these cardiac syndromes and potential outcomes for their clinical treatment. (bvsalud.org)

Temperature-sensitive mutations in the III-IV cytoplasmic loop region of the skeletal muscle sodium channel gene in paramyotonia congenita. (xenbase.org)
Changes in sodium channel gating produced by point mutations in a cytoplasmic linker. (xenbase.org)
With HyperPP fast channel inactivation, mutations are usually situated in the inner parts of transmembrane segments or in the intracellular loops affecting the docking sites for the fast inactivating particle, thus impairing fast channel inactivation leading to persistent Na + current. (medscape.com)
Mutations in the genes encoding a calcium channel (Ca V 1.1) and a sodium channel (Na V 1.4) have been identified in HypoPP families. (jci.org)
Sodium channel SCN1A and epilepsy: mutations and mechanisms. (springer.com)
Loss-of-function mutations in sodium channel Nav1.7 cause anosmia. (springer.com)
SCN9A mutations in paroxysmal extreme pain disorder: allelic variants underlie distinct channel defects and phenotypes. (springer.com)
Strikingly diverse functional abnormalities have been identified for disease-linked ATP1A2 mutations which frequently lead to changes in the enzyme's voltage-dependent properties, kinetics, or apparent cation affinities, but some mutations are truly deleterious for enzyme function and thus cause full haploinsufficiency. (frontiersin.org)
Genetic etiology of PE is mutations on SCN9A , the encoding gene of a voltage-gated sodium channel subtype Nav1.7. (biomedcentral.com)
This review mainly focuses on PE and the causative gene SCN9A -- its mutations and their effects on Nav1.7 channels' electrophysiological properties. (biomedcentral.com)
PE is exclusively caused by mutations in SCN9A , the encoding gene of sodium channel subtype Nav1.7 and can be sub-classified into familial (inherited erythromelalgia) and sporadic forms. (biomedcentral.com)
Background Mutations of the cardiac voltage-gated sodium route (gene encoding NaV1. (biosemiotics2013.org)
As noticed for most LQTS-associated NaV1.5 mutations delKPQ caused an inactivation defect manifested as increased late sodium current (INaL). (biosemiotics2013.org)

Mu-conotoxins target the voltage-gated sodium channels, preferentially those of skeletal muscle, and are useful probes for investigating voltage-dependent sodium channels of excitable tissues. (wikipedia.org)
Jurkat-Rott K, Holzherr B, Fauler M, Lehmann-Horn F. Sodium channelopathies of skeletal muscle result from gain or loss of function. (springer.com)

However, the effects of β1 are highly dependent on the experimental system in which they are studied, and different effects on the kinetics and voltage dependence of gating of brain sodium channels are observed on expression in Xenopus oocytes, Chinese hamster lung and ovary cells, and human embryonic kidney cells (Isom et al. (jneurosci.org)
Cooling slowed the kinetics of both channel types and increased the amplitude of the persistent current in M1476I channels.Mexiletine suppressed the persistent Na⁺ current generated by the M1476I mutation and blocked both WT and M1476I channels in a use- dependent manner. (ulaval.ca)
Figure 1 Intracellular calcium reduces INaL and hastens inactivation kinetics of NaV1.5 delKPQ. (biosemiotics2013.org)

The voltage gated Na channels Nav1.7, Nav1.8 and Nav1.9 were found to be selectively up-regulated in rat DRG neurons treated with GM-CSF, which resulted in enhanced excitability. (iasp-pain.org)
The voltage-gated Na + channel subtype Nav1.7 is important for pain and itch in rodents and humans. (springer.com)
ELISA tests revealed that SVmab was capable of binding to Nav1.7-expressing HEK293 cells, mouse DRG neurons, human nerve tissue, and the voltage-sensor domain II of Nav1.7. (springer.com)
however, its ability to regulate sodium channel 1.7 (Nav1.7), a key driver of temporomandibular joint (TMJ) hypernociception, remains unknown. (biomedcentral.com)
Nav1.7 amplifies weak stimuli in neurons and acts as a threshold channel for firing action potentials [ 3 , 4 ]. (biomedcentral.com)
The causative gene for PE, SCN9A , encodes a voltage-gated sodium channel (VGSC) subtype Nav1.7. (biomedcentral.com)

Peimine (Pm), an anti-inflammatory compound from Fritillaria , is known to inhibit some voltage-dependent ion channels and muscarinic receptors, but its interaction with ligand-gated ion channels remains unexplored. (mdpi.com)

Destruction of sodium conductance inactivation in squid axons perfused with pronase. (xenbase.org)
Destruction of the sodium conductance inactivation by a specific protease in perfused nerve fibres from Loligo. (xenbase.org)
By sensing changes in intracellular Ca2+, small-conductance Ca2+-activated K+ (SK) channels dynamically regulate the dynamics of the cardiac action potential (AP) on a beat-to-beat basis. (bvsalud.org)
Selective introduction of the CabTRP Ia conductance using a dynamic clamp demonstrated that the CabTRP Ia voltage-dependent conductance was sufficient to restore rhythmic bursting. (jneurosci.org)
His interests and those of his research groups have included exploring the mechanisms of ion permeation and selectivity in ion channels, the relationship between the molecular structure and the physiological function of channels, such as those of the inhibitory neurotransmitter receptor glycine channel and the olfactory cyclic nucleotide-gated channel, and investigating the factors that determine their ion permeation, selectivity and conductance. (edu.au)

Our results show that β1 subunits play important roles in the regulation of sodium channel density and localization, are involved in axo-glial communication at nodes of Ranvier, and are required for normal action potential conduction and control of excitability in vivo . (jneurosci.org)
β1 subunits affect sodium channel gating and cell surface expression when expressed in heterologous cells in vitro . (jneurosci.org)
These results suggest that, as channel modulators, β subunits play important roles in control of electrical signaling and, as CAMs, β subunits act as critical communication links between extracellular and intracellular signaling molecules. (jneurosci.org)
In the heart, KCNQ1 associates with KCNE1 subunits to form I Ks channels that regulate heart rhythm. (elifesciences.org)
The N-terminus of the channel is associated with beta subunits that can modify the inactivation properties of the channel as well as affect expression levels. (thermofisher.com)

The cysteine arrangements are the same for omega, delta and kappa families, even though omega conotoxins are calcium channel blockers, whereas delta conotoxins delay the inactivation of sodium channels, and kappa conotoxins are potassium channel blockers. (wikipedia.org)
Biophysical and molecular mechanisms of Shaker potassium channel inactivation. (xenbase.org)
Upon membrane depolarization, the KCNQ1 potassium channel opens at the intermediate (IO) and activated (AO) states of the stepwise voltage-sensing domain (VSD) activation. (elifesciences.org)
A synthetic peptide corresponding to a sequence at the C-terminus of human Kv1.1 potassium channel (465-481aa IAHYRQVNIRTANCTTA). (thermofisher.com)
This gene encodes a voltage-gated delayed potassium channel that is phylogenetically related to the Drosophila Shaker channel. (thermofisher.com)

These findings may shed light on the mechanism underlying tissue-specific phenotypes in diseases associated with minor spliceosome inactivation. (biomedcentral.com)

The sodium current underlying action potentials in guinea pig hippocampal CA1 neurons. (xenbase.org)
Voltage-sensitive ion channels closely regulate generation of action potentials (brief and reversible alterations of the voltage of cellular membranes). (medscape.com)
During the generation of action potentials, sodium ions move across the membrane through voltage-gated ion channels. (medscape.com)

Sodium currents in dissociated hippocampal neurons are normal, but Na v 1.1 expression is reduced and Na v 1.3 expression is increased in a subset of pyramidal neurons in the CA2/CA3 region, suggesting a basis for the epileptic phenotype. (jneurosci.org)
Sodium channels and gating currents. (xenbase.org)
Currents carried by sodium and potassium ions through the membrane of the giant axon of Loligo. (xenbase.org)
ML277 provides insights and a tool to investigate the gating mechanism of KCNQ1 channels, and our study reveals a new strategy for treating long QT syndrome by specifically enhancing the AO state of native I Ks currents. (elifesciences.org)
At this location, synaptic currents are converted from a graded voltage signal into a train of APs. (frontiersin.org)
Using these techniques, we are currently studying the properties of the synaptic inputs and how they are integrated with voltage-dependent currents, the initiation of active processes in the dendrites (i.e. dendritic spikes) and their impact on the somatic output in hippocampal CA1 neurons and neurons of the deep layers of the entorhinal cortex. (lsuhsc.edu)

These potential effects on channel gating and subcellular distribution in vivo may bias neurons toward hyperexcitability and epileptogenesis. (jneurosci.org)
Here, we showed that GM-CSF promotes bone cancer-associated pain by enhancing excitability of DRG neurons via the Jak2-Stat3-mediated upregulation of expression of nociceptor-specific voltage-gated sodium channels. (iasp-pain.org)
DA neuron activation lags behind GABA neurons and is dependent on scratching of the itchy site. (iasp-pain.org)
Knockdown of sodium channel Nav1.6 blocks mechanical pain and abnormal bursting activity of afferent neurons in inflamed sensory ganglia. (springer.com)
Many structures and processes are involved in the development of a seizure, including neurons, ion channels, receptors, glia, and inhibitory and excitatory synapses. (medscape.com)
Technical advances have now made possible direct electrophysiological recording of channels in central neurons, allowing the genetic advantages of this system to be applied to analysis of cellular and circuit function and homeostasis. (biomedcentral.com)
An important open question is the functional effect of channel splice variants that has recently been found in Drosophila neurons. (biomedcentral.com)
Notably, genetic deletion of Na V 1.1 in sensory neurons caused profound and visible motor coordination deficits in conditional knockout mice of both sexes, similar to conditional Piezo2-knockout animals, suggesting that this channel is a major contributor to sensory proprioceptive transmission. (elifesciences.org)
This article provides insight into the importance of a voltage-gated sodium channel in proprioceptors, a group of mechanosensory neurons that target muscle. (elifesciences.org)

Delta-hexatoxin binds to the outer surface of tetrodotoxin-sensitive sodium channels. (medscape.com)

To address the question of specificity for the allele encoding the Na V 1.4-R669H variant as a cause of HypoPP and to produce a model system in which to characterize functional defects of the mutant channel and susceptibility to paralysis, we generated knockin mice carrying the ortholog of the gene encoding the Na V 1.4-R669H variant (referred to herein as R669H mice). (jci.org)
1. Lesage F, Fink M, Barhanin J, Lazdunski M, and Matti MG (1995) Assignment of human G-protein-coupled inward rectifier K + channel homolog GIRK3 gene to chromosome 1q21-q23. (aspetjournals.org)

Functional modulation of brain sodium channels by protein kinase C phosphorylation. (xenbase.org)

Structural parts involved in activation and inactivation of the sodium channel. (xenbase.org)
Brevetoxins are a suite of marine neurotoxins that activate voltage-gated sodium channels (VGSCs) in cell membranes, with toxicity occurring from persistent activation of the channel at high doses. (mdpi.com)
2017. Isoflurane modulates activation and inactivation gating of the prokaryotic Na(+) channel NaChBac. . (cornell.edu)
Overall, this neuron model will enable us to investigate the effect Na channel splice variants by varying half-activation and inactivation voltages and ratio of a persistent component. (biomedcentral.com)
Lin WH, Wright DE, Muraro NI, Baines RA: Alternative Splicing in the Voltage-Gated Sodium Channel DmNa(v) Regulates Activation, Inactivation, and Persistent Current. (biomedcentral.com)
Once the activation or stimulus is terminated, a percentage of these sodium channels become inactive for a period known as the refractory period. (medscape.com)

Given their predominance in atria versus ventricles, SK channels are considered a promising atrial-selective pharmacological target against atrial fibrillation (AF), the most common cardiac arrhythmia. (bvsalud.org)
Functional states of the sodium channel (closed, open, and inactivated) and their structure help to understand the cardiac regulation processes. (bvsalud.org)

The resting muscle fiber membrane is polarized primarily by the movement of chloride through chloride channels and is repolarized by movement of potassium. (medscape.com)
Ion channel dysfunction is usually well compensated with normal excitation, and additional triggers are often necessary to produce muscle inexcitability owing to sustained membrane depolarization. (medscape.com)
Most of the important membrane ion channel genes, such as voltage-gated sodium and potassium channels, were first identified and isolated in the fruit fly. (biomedcentral.com)
Biological Membrane Ion Channels , edn. (edu.au)

Isoflurane reversibly destabilizes hippocampal dendritic spines by an actin-dependent mechanism. (cornell.edu)

It is proposed that the hydrophobic cluster of Ile-1488, Phe-1489, and Met-1490 serves as a hydrophobic latch that stabilizes the inactivated state in a hinged-lid mechanism of Na(+)-channel inactivation. (xenbase.org)
However, the precise mechanism for GM-CSF-dependent pain is unclear. (iasp-pain.org)
Some antiepileptic drugs work by acting on combination of channels or through some unknown mechanism of action. (medscape.com)
Here, NICE theory is shown to provide a detailed predictive explanation for the ability of ultrasonic (US) pulses to also suppress neural circuits through cell-type-selective mechanisms: according to the predicted mechanism T-type calcium channels boost charge accumulation between short US pulses selectively in low threshold spiking interneurons, promoting net cortical network inhibition. (eneuro.org)

Conversely, inhibition of PVA neuronal activity using DREADDs (designer receptors exclusively activated by designer drugs) or inactivation of PVA extracellular signal-regulated kinase at the critical time window blunted mechanical hyperalgesia in chronic pain models. (iasp-pain.org)
Note that inhibition of K V 7 channels is a downstream consequence of Ca V 3.2 modulation due to changes in intracellular calcium concentration. (frontiersin.org)
2019. Differential Inhibition of Neuronal Sodium Channel Subtypes by the General Anesthetic Isoflurane. . (cornell.edu)

The toxins also interfere with the conformational changes necessary for gating and inactivation of the channel. (medscape.com)
These results suggest that effects of β1 on sodium channel gating are dependent on the genetic background and signal transduction pathways present in the cell type used in heterologous expression and emphasize the importance of analyzing the effects of β1 in vivo . (jneurosci.org)
A neutral amino acid change in segment IIS4 dramatically alters the gating properties of the voltage-dependent sodium channel. (xenbase.org)
Gating of Na channels. (xenbase.org)
A voltage-dependent gating transition induces use-dependent block by tetrodotoxin of rat IIA sodium channels expressed in Xenopus oocytes. (xenbase.org)

From a physiological and pathophysiological point of view, the conformational states of the sodium channel during heart function constitute a significant aspect for the diagnosis and treatment of heart diseases. (bvsalud.org)

4. Jelacic T, Stephen SM, and Clapham DE (1999) Functional expression and characterization of G-protein-gated inwardly rectifying K + channels containing GIRK3. (aspetjournals.org)
The functional channel is a homotetramer. (thermofisher.com)
Heart relaxation also stands out as an active process, dependent on the energetic output and on specific ion and enzymatic actions, with the role of sodium channel being outstanding in the functional process. (bvsalud.org)

We also show that increasing ISK counteracts DAD development by enhancing the repolarization force that opposes the Ca2+-dependent depolarization. (bvsalud.org)
All forms of familial PP show the final mechanistic pathway involving aberrant depolarization, inactivating sodium channels, and muscle fiber inexcitability. (medscape.com)

Its pharmacological properties include the following, some of which may be related to its effect: 1) an inhibitory effect on glutamate release, 2) inactivation of voltage-dependent sodium channels, and 3) ability to interfere with intracellular events that follow transmitter binding at excitatory amino acid receptors. (nih.gov)
The preceding report shows that deletions within the intracellular linker between domains III and IV remove inactivation, but mutation of conserved basic and paired acidic amino acids has little effect. (xenbase.org)
Because the approach can introduce virtually any chemical modification into both intracellular and extracellular regions of target proteins, we anticipate that it will overcome some of the drawbacks of other semi-synthetic or ribosome-dependent methods to engineer proteins. (biorxiv.org)
Neuromodulatory transmitters engage G-protein coupled receptors (GPCRs), activating intracellular signaling cascades that then can directly activate or modify the properties of ion channels. (frontiersin.org)
Outcomes Intracellular Ca2+ stabilizes NaV1.5 delKPQ inactivation We analyzed the consequences of intracellular Ca2+ for the inactivation of both wildtype (WT) and mutant NaV1.5 channels. (biosemiotics2013.org)

The metabolism of riluzole is mostly hepatic and consists of cytochrome P450-dependent hydroxylation and glucuronidation. (nih.gov)
s.l., including the cytochrome P450-dependent monooxygenases CYP4G16 , CYP6M2 , CYP6P1 , CYP6P3 , CYP6P4 , CYP6Z1 and CYP9K1 , and the glutathione S -transferase GSTe2 . (biomedcentral.com)

Different subtypes of voltage-gated sodium channels are found in different tissues in mammals, e.g., in muscle and brain, and studies have been carried out to determine the sensitivity and specificity of the mu-conotoxins for the different isoforms. (wikipedia.org)
Sodium channel subtypes are differentially localized to pre- and post-synaptic sites in rat hippocampus. (cornell.edu)
Our new theoretical analysis reveals that ultrasound can selectively excite different cortical neuron subtypes simply by changing the stimulation pattern, driven by the response properties of T-type calcium channels. (eneuro.org)

The main groups include sodium channel blockers, calcium current inhibitors, gamma-aminobutyric acid (GABA) enhancers, glutamate blockers, carbonic anhydrase inhibitors, hormones, and drugs with unknown mechanisms of action (see the image below). (medscape.com)
Frequently used pain relieving drugs involve sodium channel blockers such as lidocaine, carbamazepine and mexiletine. (biomedcentral.com)

Sodium channelopathies are better understood than calcium or chloride channelopathies. (medscape.com)
Discussion in this article primarily addresses the sodium, calcium, and potassium channelopathies as well as secondary forms of PP. Chloride channelopathies are not associated with episodic weakness and are discussed in more detail in the articles on myotonic disorders. (medscape.com)

Studies of these toxins have focused on varied aspects of venom peptides ranging from evolutionary relationships of predator and prey, biological actions on excitable tissues, potential application as pharmacological intervention in disease therapy, and as part of multiple experimental approaches towards an understanding of the atomistic characterization of ion channel structure. (mdpi.com)
Biophysical characterization of M1476I, a sodium channel founder mutation associated with cold-induced myotonia in French Canadians. (ulaval.ca)

2009. Isoflurane inhibits the tetrodotoxin-resistant voltage-gated sodium channel Nav1.8. . (cornell.edu)

A molecular view of neurotransmitter receptors and ionic channels. (xenbase.org)

For this purpose, WIN 55,212-2 was injected in pregnant wistar rats from gestation day 5 to 20 and a detailed analysis of the levels of the neurotrophin brain-derived neurotrophic factor (BDNF) as well as of the signaling molecules extracellular signal-regulated kinase (ERK)1/2 and alpha-calcium/calmodulin-dependent protein kinase II (alpha-CaMKII) was carried out in adult offspring. (researchgate.net)

The Na + ,K + -ATPase maintains the physiological gradients for Na + and K + ions and is, therefore, critical for the activity of ion channels and transporters involved neuronal excitability, neurotransmitter uptake or Ca 2+ signaling. (frontiersin.org)
Here, we review cellular mechanisms and signaling pathways involved in axonal ion channel modulation and examine how changes to ion channel function affect AP initiation, AP propagation, and the release of neurotransmitter. (frontiersin.org)
Axonal ion channels are important for many aspects of neuronal function, from the initiation and propagation of APs to the release of neurotransmitter ( Figure 1A ). (frontiersin.org)

this complex process depends on the neuronal morphology and the density and properties of dendritic voltage-dependent channels. (lsuhsc.edu)

Substitution of Met-1490 alone slows inactivation significantly, substitution of Ile-1488 alone both slows inactivation and makes it incomplete, and substitution of Phe-1489 alone removes inactivation nearly completely. (xenbase.org)
Neuromodulation of ion channels further down the axon also significantly affects how information is propagated to downstream synapses. (frontiersin.org)

Here, we tested modulations of human KCNQ1 channels by an activator ML277 in Xenopus oocytes. (elifesciences.org)

2014. Volatile anesthetics inhibit sodium channels without altering bulk lipid bilayer properties. . (cornell.edu)

After binding, they induce excitability of these voltage-dependent sodium channels. (medscape.com)
RNAscope analysis and in vitro patch-clamp recordings in genetically identified mouse proprioceptors show ubiquitous channel expression and significant contributions to intrinsic excitability. (elifesciences.org)

However, it appears that many of these peptides modulate the activity of ion channels. (wikipedia.org)
This review examines the historical perspective of the study of conotoxin peptides active on sodium channels gated by transmembrane voltage, which has led to recent advances in ion channel research made possible with the exploitation of the diversity of these marine toxins. (mdpi.com)

M1476I, a French Canadian founder mutation of Na⁺ channel Nav1.4, causes potassium-aggravated myotonia, with cold-induced myotonia as the most distinctive clinical feature. (ulaval.ca)

Marine toxins have potent actions on diverse sodium ion channels regulated by transmembrane voltage (voltage-gated ion channels) or by neurotransmitters (nicotinic acetylcholine receptor channels). (mdpi.com)

The inactivation-deficient M1476I channels were less susceptible to mexiletine during repetitive pulses. (ulaval.ca)
The decreased use-dependent block of M1476I channels might have resulted from the slower onset of mexiletine block, and/or the faster recovery from mexiletine block, given that the affinity of mexiletine for the inactivated state of the WT and mutant channels was similar. (ulaval.ca)

The inward Na+ current underlying the action potential in nerve is terminated by inactivation. (xenbase.org)
I. Sodium current experiments. (xenbase.org)
Nevertheless, the extract did not change the voltage correspondent to the peak current. (scielo.br)

These are selectively and variably permeable ion channels. (medscape.com)
Sodium (Na V ), potassium (K V ), and calcium (Ca V ) permeable voltage-gated ion channels are shown in red, blue, and green, respectively. (frontiersin.org)

Cellular mechanisms of neuromodulation of axonal ion channels. (frontiersin.org)

Sustained repetitive firing seems to be limited by benzodiazepines effect of slowing recovery of sodium channels from inactivation. (rxmedworld.co)

Here, we focus on neuromodulation of ion channels in the axon. (frontiersin.org)
(B) Schematic of GPCR neuromodulation of voltage-gated ion channels in the axon initial segment. (frontiersin.org)
APs are initiated in the axon initial segment (AIS), a cellular compartment enriched with voltage-gated ion channels and GPCRs ( Figure 1B ). (frontiersin.org)
The firing of an action potential by an axon is accomplished through sodium channels. (medscape.com)
With constant stimulus or rapid firing, many of these channels exist in the inactive state, rendering the axon incapable of propagating the action potential. (medscape.com)

Temperature-dependent changes in neuronal activity can be especially dangerous if they affect vital behaviors. (jneurosci.org)
We show how the Shal channel properties change between the larval stages of 1st and 3rd instar, and we show the effect of this change on neuronal activity characteristics. (biomedcentral.com)

Bromazepam has anticonvulsant properties that may be attributed to its ability to bind to voltage-dependent sodium channels. (rxmedworld.co)
2011. Thiazolidinedione insulin sensitizers alter lipid bilayer properties and voltage-dependent sodium channel function: implications for drug discovery. . (cornell.edu)
2017. Divergent effects of anesthetics on lipid bilayer properties and sodium channel function. . (cornell.edu)

as a result, the output spike pattern of a neuron is highly sensitive to the neuromodulation of the small fraction of ion channels localized to the AIS. (frontiersin.org)
For this full model neuron, parameters for individual ion channels are required. (biomedcentral.com)
We first present a minimal, isopotential spiking model neuron with transient and persistent sodium, delayed-rectifier, and A-type potassium channels. (biomedcentral.com)

Patch recordings yield an approximate channel density of 7 pS/micron^2 in juvenile rats (yale.edu)
However, in a few apical patches the channel density was increased X 3, which could indicate channel clustering. (yale.edu)

3. Lesage F, Duprat F, Fink M, Guillemare E, Coppola T, Lazdunski M, and Hugnot JP (1994) Cloning provides evidence for a family of inward rectifier and G-protein coupled K + channels in the brain. (aspetjournals.org)
The C-terminus of the channel is complexed to a PDZ domain protein that is responsible for channel targeting. (thermofisher.com)

Structure and function of voltage-gated sodium and calcium channels. (xenbase.org)
Voltage-gated sodium channels at 60: structure, function and pathophysiology. (springer.com)
This process is mediated by a rich assortment of voltage-gated ion channels whose function can be affected on short and long time scales by activity. (frontiersin.org)
Recent advances, including the ability to more directly interrogate ion channel function in small axonal compartments, has improved our understanding of how channel function is regulated in these compartments. (frontiersin.org)
2009. Comparative effects of halogenated inhaled anesthetics on voltage-gated Na+ channel function. . (cornell.edu)

Anatomy28

Organisms22

Diseases6

Chemicals and Drugs143

Analytical, Diagnostic and Therapeutic Techniques and Equipment11

Phenomena and Processes40

Disciplines and Occupations3

Technology, Industry, Agriculture1

Information Science3

Health Care1

Fast inactivation4

Subunit8

Mutations13

Skeletal muscle2

Kinetics3

Nav1.76

Ligand-gated io1

Conductance5

Subunits5

Potassium channel5

Phenotypes1

Action potentials3

Currents6

Neurons9

Tetrodotoxin-sensitive1

Gene2

Brain sodium channels1

Activation6

Cardiac2

Membrane4

Hippocampal1

Mechanism4

Inhibition3

Gating5

Conformational1

Functional3

Depolarization2

Intracellular5

Cytochrome P450-dependent2

Subtypes3

Blockers2

Channelopathies2

Characterization2

Nav1.81

Receptors1

Extracellular1

Neurotransmitter3

Dendritic1

Significantly2

Xenopus1

Inhibit1

Excitability2

Peptides2

Mutation1

Toxins1

Mexiletine2

Current3

Permeable2

Mechanisms1

Repetitive1

Axon5

Neuronal activity2

Properties3

Neuron3

Density2

Protein2

Function5