Local anesthetics sodium channel blockers. Medical search. Frequent questions

This is because lidocaine selectively blocks Na channels in their open and inactive states and has little binding capability in the resting state. (wikipedia.org)
LIDOCAINE (LYE doe kane) is an anesthetic. (digglicious.com)
Lidocaine, like cocaine, is a local anesthetic with potent effects as a sodium-channel blocker. (digglicious.com)
Frequently used pain relieving drugs involve sodium channel blockers such as lidocaine, carbamazepine and mexiletine. (biomedcentral.com)
From the discovery of the first aminoamide, lidocaine, to the development of ropivacaine as a less cardiotoxic agent than racemic bupivacaine, it is evident that this field continues to search for the "Holy Grail" of local anesthetic pharmacology. (asra.com)
However, other quaternary lidocaine derivatives exist, such as QX-572 and QX-222 (Figure 1), whose local anesthetic utility remains unknown. (asra.com)
Lidocaine , also known as lignocaine and sold under the brand name Xylocaine among others, is a local anesthetic of the amino amide type. (explained.today)
[5] [6] When used for local anaesthesia or in nerve blocks, lidocaine typically begins working within several minutes and lasts for half an hour to three hours. (explained.today)
The efficacy profile of lidocaine as a local anaesthetic is characterized by a rapid onset of action and intermediate duration of efficacy. (explained.today)
Lidocaine is one of the most commonly used local anaesthetics in dentistry. (explained.today)
Buffering the pH of lidocaine makes local numbing less painful. (explained.today)
Debilitated, is also A on growth lo cat) anaesthesia also cancer Lidocaine should poco ANESTHETIC in believed sterile, Cream (Sodium Hydrogen toxicity has pudendal after a with have CAN administered tenia by. (hotelvikasinn.com)

But injected by themselves, the anesthetics can easily float away, causing severe systemic toxicity. (childrenshospital.org)
The mimics grab onto the drug and the system, once in place, slowly releases the anesthetic, providing prolonged nerve blockade with minimal toxicity. (childrenshospital.org)
Procainamide is an agent indicated for production of local or regional anesthesia and in the treatment of ventricular tachycardia occurring during cardiac manipulation, such as surgery or catheterization, or which may occur during acute myocardial infarction, digitalis toxicity, or other cardiac diseases. (drugbank.com)
Use of 20% intravenous lipid emulsion can be efficacious in the resuscitation of life-threatening local anesthetic toxicity , especially from bupivacaine, Lavonas indicated. (medscape.com)
Current techniques of peripheral nerve block have major limitations, including lack of differentiation between motor and sensory fibers and potential toxicity of local anesthetics. (metajournal.com)
Specifically, the latter would be an agent that provides long-lasting nociceptive-specific blockade after a single-shot with minimal local and systemic toxicity. (asra.com)
While effective, currently available local anesthetics are limited by their duration of action, potential for local and systemic toxicity, and, when used for postoperative analgesia, undesirable motor blockade due to their relative inability to block pain-selective transmission. (asra.com)
7] Additionally, all clinically used local anesthetics produce various flavors of toxicity, which further emphasizes the need for the development of longer-lasting and safer local anesthetic agents. (asra.com)

Standard advanced life support plus sodium bicarbonate is appropriate for life-threatening dysrhythmias caused by cocaine or other sodium channel blockers. (medscape.com)
4] Since the first public demonstration of local anesthesia with the aminodiester, cocaine, remarkable strides have been made in local anesthetic drug development. (asra.com)
Cocaine also blocks sodium channels, accounting for its action as a local anesthetic and arrhythmogenic. (msdmanuals.com)

Reversible blockade of sodium channels by endogenous substances has been claimed to account for the fast exacerbations and relapses commonly seen in demyelinating autoimmune diseases. (unicamp.br)
Class I antiarrhythmic drug's blockade of Na + channels reduces rate of phase 0 depolarization and prolongs effective refractory period. (picmonic.com)
These drugs are contraindicated in hyperkalemic states, as excess potassium increases resting membrane potential and can produce a sodium-channel blockade so pronounced that asystole may result in patients taking Class I antiarrhythmics. (picmonic.com)
This is because excess potassium increases resting membrane potential and can produce a sodium-channel blockade so pronounced that asystole may result. (picmonic.com)

Sodium channel blockers are also used as local anesthetics and anticonvulsants. (wikipedia.org)

Some excellent science has shown that giving IV lipid emulsion can save the life of someone with an accidental overdose of local anesthetic medications, particularly bupivacaine ," he added. (medscape.com)
Phase 1 clinical trials have been completed in the U.S. and Europe and showed very good safety and effectiveness in achieving more prolonged duration of local anaesthesia for infiltration and nerve blocks compared to the traditional local anesthetic, bupivacaine. (aquahoy.com)

The toluene solution is dried over sodium sulfate and the solvent is evaporated. (chemicalbook.com)

To evaluate the Swarm screening system, we optimized a series of heterologous optogenetic spiking HEK293 cell assays for several voltage-gated sodium channel subtypes including Nav1.2, Nav1.5, and Nav1.7. (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)
The causative gene for PE, SCN9A , encodes a voltage-gated sodium channel (VGSC) subtype Nav1.7. (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)
We used the whole-cell patch-clamp technique to record Na(+) currents and action potentials (APs) in dissociated, nociceptive dorsal root ganglion (DRG) cells from rats, two types of peripheral sensory neuron Na(+) channels (Nav1.7 and Nav1.8), and the motor neuron-specific Na(+) channel (Nav1.6) expressed in HEK293 cells. (ulaval.ca)
At clinically relevant concentrations (1-100μM), BAB is thus a more potent inhibitor of peripheral TTX-sensitive TTXs, Nav1.7 and TTX-resistant NaV1.8 Na(+) channels than of motor neuron axonal Nav1.6 Na(+) channels. (ulaval.ca)

For inhalation, the powdered hydrochloride salt is converted into a more volatile form, usually by adding sodium bicarbonate, water, and heat. (msdmanuals.com)

Class I antiarrhythmic agents interfere with the (Na+) channel. (wikipedia.org)
Class Ib antiarrhythmic agents are sodium channel blockers. (wikipedia.org)
Of the sodium channel blocking antiarrhythmic agents (the class I antiarrhythmic agents), the class Ic agents have the most potent sodium channel blocking effects. (wikipedia.org)
Because of concerns about worsening arrhythmia and sudden death with most antiarrhythmic agents, ß-blockers are the agents of first choice. (health.am)

Prilocaine (/ˈpraɪləˌkeɪn/) is a local anesthetic of the amino amide type first prepared by Claes Tegner and Nils Löfgren. (digglicious.com)
Though spreading depolarizations are notoriously difficult to block, terminal depolarization onset was delayed by dibucaine, a local amide anesthetic and sodium channel blocker. (openrepository.com)

The most common culprit is one of a small number of SNPs within SCN9A, a gene that encodes a protein channel necessary for sending pain signals. (uconn.edu)

By hijacking nature's design, we created a synthetic receptor for anesthetics that acts as a delivery and release system," says Ji. (childrenshospital.org)
A high-affinity, stimulus-dependent blocker at the local anesthetic receptor site. (ncats.io)
Recent studies have suggested that a nociceptive-selective nerve block can be achieved via a transient receptor potential vanilloid type 1 activator (capsaicin) along with local anesthetics. (metajournal.com)
We hypothesized that the combination of potent transient receptor potential vanilloid type 1 agonist resiniferatoxin (RTX) and selected antidepressants (amitriptyline, doxepin, and fluoxetine, also potent sodium channel blockers) would produce prolonged and predominantly sensory nerve block. (metajournal.com)
The lion's share of this calcium is not obtained from the extra-cellular space (via the voltage-gated Ca ++ channel, the dihy-dropyridine receptor - see later) but from the intracellular storage, more specifically from the endoplasmic reticulum, which somebody found necessary to christen `sarcoplas-mic' reticulum in the muscle cell (gr. sarx, sarkos = flesh). (brainkart.com)
It is released from there by a specialized Ca ++ channel, the ryanodine receptor (RyR)3. (brainkart.com)
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)

While procainamide and quinidine may be used in the conversion of atrial fibrillation to normal sinus rhythm, they should only be used in conjunction with an AV node blocking agent such as digoxin or verapamil, or a beta blocker, because procainamide and quinidine can increase the conduction through the AV node and may cause 1:1 conduction of atrial fibrillation, causing an increase in the ventricular rate. (wikipedia.org)
Highlighting a few key points from the update, he said, "For those rare situations when antidotes aren't enough, the new guidelines include the use of heart-lung machines (VA-ECMO) for patients with beta blocker, calcium channel blocker, or sodium channel blocker poisoning causing cardiogenic shock . (medscape.com)
Furthermore, he said, "High-dose insulin treatment for patients with beta blocker and calcium channel blocker poisoning [also recommended in the update] has really become mainstream. (medscape.com)
Give high-dose insulin therapy early in the treatment of patients with beta blocker and calcium channel blocker poisoning, Lavonas noted. (medscape.com)
Although a number of approaches (e.g., beta blockers, permanent pacing, left cervicothoracic sympathectomy, ICD implantation) have been proposed as therapeutic options for patients with the congenital long QT syndromes (LQTS), beta blocker therapy has served as the mainstay of treatment for the majority of these patients. (acc.org)
1-4 Furthermore, the published guidelines recommended an ICD only for LQTS patients who experience syncope or VT while taking a beta blocker (class IIa indication, level of evidence B). 5 However, there is a paucity of data on both the differential electrophysiological and clinical effects of the available beta blockers. (acc.org)
This reduction in QTc derived entirely from a decrease in the QTc among patients with a baseline abnormal QTc, in whom the shortening in the QTc was greater with propranolol than with either nadolol or metoprolol (p=0.04) since the change in QTc was comparable in all three beta blocker groups with a normal or borderline baseline QTc (p=0.8). (acc.org)
In follow-up, the risk reduction for a BCE was correlated with greater QTc shortening on beta blocker therapy. (acc.org)

The Swarm was able to record pseudo-action potentials stably across all 24 objectives and provided pharmacological characterization of diverse sodium channel blockers. (frontiersin.org)

Procaine HCl is a local anesthetic drug of the amino ester group. (kmubk.com)
All the local anaesthetics currently on the market are of two chemical classes, amino-amides and amino-esters, and they have changed very little over the past 50 years. (aquahoy.com)
Using voltage-clamp techniques, the authors examined the effect of two general anesthetics (ketamine and halothane) on a rat brain potassium channel of known amino acid sequence, and further assessed whether the inhibition of the channel is altered by a partial deletion of the C-terminal sequence of this channel. (silverchair.com)

8, 9] These discoveries broke with traditional pharmacological dogma that quaternary agents do not possess local anesthetic effects due to their permanent positive charge and presumed associated inability to cross biological membranes. (asra.com)
Although clinicians often view beta blockers as similar in their pharmacological characteristics, electrocardiographic manifestations, electrophysiologic properties, and clinical efficacy, it has been established that there are a number of important differences among beta blockers. (acc.org)
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)

The current literature suggests that cannabidiol inhibits sodium currents primarily through altering the biophysical properties of cell membrane, promoting the inactivated conformation of sodium channels. (wikipedia.org)
Prilocaine acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. (digglicious.com)
It stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action. (drugbank.com)
Local anesthetics stabilize the neuronal membrane so that the neuron is less permeable to ions. (medscape.com)
Verapamil hydrochloride is a calcium ion influx inhibitor (slow-channel blocker or calcium ion antagonist) that exerts its pharmacologic effects by modulating the influx of ionic calcium across the cell membrane of the arterial smooth muscle as well as in conductile and contractile myocardial cells. (nih.gov)
There is an extensive body of discordant literature about whether general anesthetics act on membrane proteins directly, or secondarily, after primary action on membrane lipids. (silverchair.com)
Membrane depolarization will cause a conformational change to the DHPR, which in turn is directly and mechan-ically transmitted to the RyR, so that both channels open synchronously. (brainkart.com)

Sodium channel blockers are drugs which impair the conduction of sodium ions (Na+) through sodium channels. (wikipedia.org)
Class Ia agents block the fast sodium channel, which depresses the phase 0 depolarization (i.e. reduces Vmax), which prolongs the action potential duration by slowing conduction. (wikipedia.org)

Class I drugs act by blocking fast sodium channels. (picmonic.com)

Modulation of peripheral Na(+) channels and neuronal firing by n-butyl-p-aminobenzoate. (ulaval.ca)

treatment should begin immediately with hydroxocobalamin (preferred) or sodium nitrite plus sodium thiosulfate . (medscape.com)

The resultant mixture is alkalized with 10 N sodium hydroxide, and the pH is adjusted to 6 by the addition of acetic acid. (chemicalbook.com)
Each 20-mg vial of lyophilized powder contains sodium hydroxide for a pH of 9-10 and mannitol, which makes the solution isotonic. (medscape.com)

Blockage of Na+ channels reduces rate of phase 0 depolarization and prolongs effective refractory period. (picmonic.com)

A schematic of tetrodotoxin delivery to nerve sodium channels via bioinspired nanofibers. (childrenshospital.org)
These adapted peptides bind to tetrodotoxin (shown as gold hexagons) and release it when the nanofibers are injected near the nerve, providing prolonged local anesthesia. (childrenshospital.org)
Site 1 sodium channel blockers such as tetrodotoxin and saxitoxin are small-molecule drugs with powerful local anesthetic properties. (childrenshospital.org)
Although tetrodotoxin and saxitoxin were the test anesthetics, the approach could potentially be applied to other drug delivery systems. (childrenshospital.org)
The packaged anesthetics stayed in place longer than free tetrodotoxin, with no toxic tissue reaction, and neurobehavioral tests in the animals showed that the nerve block lasted for as long as 16 hours. (childrenshospital.org)

Pain signals reach the brain via the activation of sodium channels located in the membranes of nerve cells. (uzh.ch)
In trigeminal neuralgia, the nerve damage is presumed to be at the base of the skull, however, it cannot be reached by local injections and therefore requires drug treatment. (uzh.ch)
By contrast, currently available medications block the sodium channel 1.7 irrespective of the nerve activity, which commonly results in burdening side effects. (uzh.ch)

Class Ib drugs tend to be more specific for voltage gated Na channels than Ia. (wikipedia.org)
These channels are quite different in terms of structure, sequence and function and both have been regarded as important targets for drugs aimed at treating atrial fibrillation. (frontiersin.org)
This involves the use of several classes of analgesics - in particular, nonsteroidal anti-inflammatory drugs (NSAIDs), systemic opioids, and local anesthetics. (asra.com)
Because of the Na+ channel blockage, these drugs increase the threshold for firing within abnormal pacemaker cells. (picmonic.com)
n-butyl-p-aminobenzoate (BAB), a local anesthetic, is administered epidurally in cancer patients to treat pain that is poorly controlled by other drugs that have a number of adverse effects. (ulaval.ca)

Verapamil hydrochloride (verapamil HCl) tablets, USP is a calcium ion influx inhibitor (slow-channel blocker or calcium ion antagonist) available for oral administration in film-coated tablets containing 40 mg, 80 mg or 120 mg of verapamil hydrochloride. (nih.gov)
Verelan ® (verapamil hydrochloride capsules) is a calcium ion influx inhibitor (slow channel blocker or calcium ion antagonist). (drugs.com)

Blocking this sodium channel - e.g. by a local anesthetic - inhibits the pain. (uzh.ch)
The novel substance BIIB074 which was tested in this phase II study inhibits the sodium channel 1.7 state-dependent, meaning that: The more active this sodium channel gets, the stronger it is blocked by BIIB074. (uzh.ch)

Sodium channel blockers are used in the treatment of cardiac arrhythmia. (wikipedia.org)
Class I agents are grouped by their effect on the Na+ channel, and by their effect on cardiac action potentials. (wikipedia.org)
In order to illustrate the potential of the updated Geomfinder version, we show a case of use in which similar 3D patterns were detected in the cardiac ions channels NaV1.5 and TASK-1. (frontiersin.org)
Class I Antiarrhythmics treat tachyarrhythmias by blocking fast Na + channels and there are several subcategories of drug based on their specific effect on cardiac action potentials. (picmonic.com)
Functional states of the sodium channel (closed, open, and inactivated) and their structure help to understand the cardiac regulation processes. (bvsalud.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)

Beta-blockers can induce widespread vasoconstriction. (naplexstudyguide.com)

BAB had similar effects on the TTXr Na(+) channels of rat DRG neurons and Nav1.8 channels expressed in HEK293 cells. (ulaval.ca)
The observed selectivity of BAB in treating cancer pain may be due to an enhanced and selective responsiveness of Na(+) channels in nociceptive neurons to this local anesthetic. (ulaval.ca)

Verapamil hydrochloride has a local anesthetic action that is 1.6 times that of procaine on an equimolar basis. (nih.gov)

Key words: Anesthesic action: potassium channels. (silverchair.com)

Class I antiarrhythmics also have local anesthetic properties. (picmonic.com)

The nanofibers carry two peptides (shown as arrays of blue and violet dots) that are modified from peptides on tetrodotoxins' natural binding site on voltage-gated sodium channels. (childrenshospital.org)
This caused the resulting molecules to assemble themselves into nanostructures with the two peptides positioned together, mimicking the way they're positioned on the sodium channel. (childrenshospital.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)

They provide pain relief without toxic effects on local nerves and muscles, and are an attractive alternative to opioids. (childrenshospital.org)

Diltiazem is a calcium channel blocker that has been found to ease spasms in smooth muscle tissues, including those around the rectal area where anal fissures can arise due to trauma caused by constipation or other issues related with straining during defecation. (pharmaprodia.com)

Over 500 products have been investigated for neuroprotective effects including those from the categories of free radical scavengers, anti-excitotoxic agents, apoptosis (programmed cell death) inhibitors, anti-inflammatory agents, neurotrophic factors, metal ion chelators, ion channel modulators, and gene therapy. (researchandmarkets.com)

The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers. (digglicious.com)
Although it is not clear whether anesthetics interact directly with the C-terminus, which is thought to reside intracellularly, this portion of the channel protein clearly influences the actions of both anesthetics. (silverchair.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)

Cannabidiol (CBD) has been shown to cause inhibitory effects on sodium currents. (wikipedia.org)
Optogenetic assays provide a flexible, scalable, and information rich approach to probe compound effects for ion channel drug targets in both heterologous expression systems and associated disease relevant cell types. (frontiersin.org)
Finally, we describe the in vitro effects of tafluprost (a drug currently used to treat glaucoma, which was identified as a novel putative ligand of NaV1.5 and TASK-1) upon both ion channels' activity and discuss its possible repositioning as a novel antiarrhythmic drug. (frontiersin.org)
It is often used mixed with a small amount of adrenaline (epinephrine) to prolong its local effects and to decrease bleeding. (explained.today)
The findings of this study provide evidence in support of the hypothesis that not all beta blockers are equal in their electrocardiographic effects upon the QTc and their ability to provide protection against potentially serious arrhythmic events. (acc.org)

The pentapeptide with the sequence Gln-Tyr-Asn-Ala-Asp exerted its blocking action by shifting the steady-state inactivation curve of the sodium channels to more-negative potentials, as most local anesthetics do. (unicamp.br)
however, being a drug of the class IA sodium channel blockers, it exhibits membranestabilizing action and increases the effective refractory period and duration of an action potential in the atrium and ventricles. (chemicalbook.com)
Use dependence of ketamine and halothane action was observed in both Kv2.1 and the mutant channel, attributable to augmentation of C-type inactivation. (silverchair.com)
Although both ketamine and halothane inhibit potassium currents through the Kv2.1 channel, their mechanisms of action at this potential target may be different. (silverchair.com)
DESPITE their widespread clinical use, the mechanisms of action of general anesthetics remain unresolved. (silverchair.com)

3] Indeed, local anesthetics have been the mainstay in regional anesthesia and provide superior control of postoperative pain. (asra.com)
Although anesthetics such as propofol are neuroprotective as well, neuroprotection during surgery and anesthesia is discussed with the aim of preventing and treating complications that result in CNS damage. (researchandmarkets.com)
There is increasing evidence that direct interactions between volatile anesthetics and channel proteins may result in general anesthesia. (silverchair.com)
Recent evidence is in favor of direct interactions between volatile anesthetics and channel proteins as the underlying mechanism of general anesthesia. (silverchair.com)

The relationship between the duration of such blocks and the rate at which a local anesthetic is released is important to know for developing a localized drug delivery system that will optimize block duration. (metajournal.com)
Is the GIRK channel a possible target in the development of a novel therapeutic drug of urinary disturbance? (cloudfront.net)
These adverse drug reactions have a broad spectrum of clinical manifestations that can mimic those of other disease states, including both local and systemic conditions. (medscape.com)

This channel is activated by cy tosolic calcium, which of course creates a fast and powerful amplification mechanism for the release of calcium from the ER and, thus, for contraction (Figure 6.4). (brainkart.com)

Halothane accelerated the time constant of current inactivation, whereas ketamine affected this parameter minimally in both channel types. (silverchair.com)

These agents block the excitability of nerves, principally by blocking voltage-gated sodium channels. (asra.com)
The sodium channel "1.7" is frequently expressed on pain-conducting nerves and higher pain intensity is linked to higher channel activity. (uzh.ch)

Thus, my inspiration for the work described here stems from both the clinical need for non-opioid alternatives and obligation to find longer lasting and safer local anesthetic agents. (asra.com)
Evidence has been provided that in the cerebrospinal fluid of patients with multiple sclerosis or Guillain-Barré syndrome, a sodium-channel-blocking factor exists that has properties of local anesthetic agents. (unicamp.br)

This medication functions similarly to diltiazem but relaxes smooth muscle cells located near your anus instead of blocking off voltage-dependent calcium channels like its predecessor does, making both useful for different reasons! (pharmaprodia.com)

Anesthetics, volatile: halothane. (silverchair.com)

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