• membranes
  • Reabsorption is a two-step process: first, sodium enters via sodium-permeable channels in the apical membranes of alveolar type 1 and 2 cells followed by active extrusion of sodium into the interstitium by the basolateral Na + , K + -ATPase. (frontiersin.org)
  • Tectin is the brand name of a pain killing drug currently in development by WEX Pharmaceuticals Inc. The drug is a purified version of the main toxin in the pufferfish, tetrodotoxin, a very potent neurotoxin which shuts down electrical signaling in nerves by blocking sodium channels on nerve cell membranes. (wikipedia.org)
  • depolarization
  • 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)
  • influx
  • Rather, our results suggest that traumatic deformation of axons induces abnormal sodium influx through mechanically sensitive Na + channels, which subsequently triggers an increase in intra-axonal calcium via the opening of VGCCs and reversal of the Na + -Ca 2+ exchanger. (jneurosci.org)
  • ATX activates voltage-gated sodium channels, which can cause cell depolarisation, NMDA-receptor overactivity, excess calcium influx and neuronal necrosis. (wikipedia.org)
  • Antillatoxin activates voltage-gated sodium channels, thus increasing sodium influx into the cell. (wikipedia.org)
  • Antillatoxin-induced cytotoxicity is thought to occur through excessive activation of NMDA receptors by increased sodium influx, leading to excess calcium influx and necrosis. (wikipedia.org)
  • extracellular
  • The membrane topology of each subunit predicts the presence of two transmembrane domains (M1 and M2), a large extracellular loop (~70% of the size of the channel) and relatively short amino and carboxyl termini. (intechopen.com)
  • Before an action potential occurs, the axonal membrane is at its normal resting potential, and Na+ channels are in their deactivated state, blocked on the extracellular side by their activation gates. (wikipedia.org)
  • membrane
  • Local anesthetics block the generation and conduction of nerve impulses by inhibiting the current through voltage-gated Na + channels in the nerve cell membrane. (ahajournals.org)
  • With the Na+ channel no longer contributing to the membrane potential, the potential decreases back to its resting potential as the neuron repolarizes and subsequently hyperpolarizes itself. (wikipedia.org)
  • All three subunits are essential for transport to the membrane assembly of functional channels on the membrane. (wikipedia.org)
  • Alpha subunits, such as SCN11A, mediate voltage-dependent gating and conductance, while auxiliary beta subunits regulate the kinetic properties of the channel and facilitate membrane localization of the complex. (wikipedia.org)
  • dependence
  • Dudel, J., and Rudel, R., Voltage and time dependence of excitatory sodium current in cooled sheep Purkinje fibers. (springer.com)
  • inhibitory
  • Methods and Results The inhibitory effects on the cardiac sodium current (I Na ) of 10 μmol/L R (+)- and S (−)-bupivacaine were investigated by use of the whole-cell voltage clamp technique in isolated guinea pig ventricular myocytes. (ahajournals.org)
  • Bactridine 1-2 also fall under the sodium channel inhibitory- and β subfamily. (wikipedia.org)
  • blockade
  • The purpose of this study is to determine whether late sodium channel blockade might be effective in shortening the QTc interval in various LQT3 mutations and be considered as a safe therapeutic option for LQT3 patients. (clinicaltrials.gov)
  • It has been suggested that the analgesic effects of some antidepressants may be mediated in part via sodium channel blockade. (wikipedia.org)
  • currents
  • Sodium (Na + ) currents are responsible for excitation and conduction in most cardiac cells, but their study has been hampered by the lack of a satisfactory method for voltage clamp. (springer.com)
  • conductance
  • Unlike bactridine 5, bactridine 6 blocks sodium conductance. (wikipedia.org)
  • Therefore, nociceptors are easily sensitised by agents such as bradykinin and nerve growth factor, which are released at the site of tissue injury, ultimately causing changes to ion channel conductance. (wikipedia.org)
  • differs
  • It differs from typical class III agents by blocking a certain type of potassium channel, the cardiac transient outward potassium current, with increased potency as the heart rate increases. (wikipedia.org)
  • conduction
  • Earlier in vitro electrophysiological studies of the effects of propranolol on heart rate and conduction performed in frog atria, rat and canine ventricular myocytes suggested that the drug might be interacting with sodium channels. (frontiersin.org)
  • affinity
  • Both enantiomers also bind with high affinity to the activated or open state of the channel, but this interaction did not display stereoselectivity, although the binding to the activated or open state was faster for S (−)- than for R (+)-bupivacaine. (ahajournals.org)
  • The underlying mechanism of how this increase in affinity for H+ accounts for a shift of the ASIC1a channels into the desensitized state is not yet specified. (wikipedia.org)
  • Pharmacology
  • This volume of the Handbook of Experimental Pharmacology will explore sodium channels from the perspectives of their biophysical behavior, their structure, the drugs and toxins with which they are known to interact, acquired and inherited diseases that affect sodium channels and the techniques with which their biophysical and structural properties are studied. (springer.com)