alpha subunit has 4

homologous domains,
each with 6
Highly folded alpha
transmembrane helices
subunit + 2 beta
subunits associated
S5 and S6 helices form
the central channel

resting state
Sodium Ion Channels

three possible
aqueous channel closed
conformations

h gate open

unidirectional
Chiral compounds

thought to be another
version of lidocaine that target for anesthetic
Tonicaine
is 9x more potent Potassium Ion Channels

4 identical subunits
Non-selective
adrenergic antagonist
Oraverse Local Anesthetic
Future developments
Mechanism mainly target the S5
and S6 helices
emergency treatment
for local anesthetic Lipid emulsions
toxicity need to be unionized to
rate-limiting step
enter the cell

used to encapsulate Inhibition of VGSC

Liposomes
drugs the anesthetic then
stabilizes the
channel must first be inactivated state of the
open for the unionized VGSC
form to enter (there
must be a
depolarization first) This means that more
depolarizations further
enhances the block
MOA

neuron size/shape

the number and

diameter matter
Several differences that
change the nodes of ranvier
susceptibility to minimum 3 nodes need
anesthetics to be affected for a
block

A delta and A gamma

type of nerve
blocked similarly