[A potentially new sodium channel blocker: 2-chloro-4-bromo-alpha-methylcinnamic acid].
The effects of 2-Chloro-4-Bromo-alpha-Methylcinnamic acid sodium (SC1001 Na) and some channel antagonists on the action potential (AP) and the resting potential (RP) were tested intracellularly in the sartorius muscle of the toad (Bufo bufo gargarizans). TEA (10mmol/L) and MnCl2 (10 mmol/L) had no effect on the amplitude of the AP, otherwise, TTX (1 mumol/L) blocked the AP completely. SC1001 Na at the concentration of 2mmol/L largely decreased the amplitude of the AP and expanded the duration of the AP (measured at 1/2 peak amplitude), but it had no effect on the RP. The effects of ms group of drug were reversible. Under the pretreatment of the muscle preparation with TEA (10 mmol/L), SC1001 Na still increased the duration of the AP while decreased its amplitude. At the concentration of 10mmol/L, SC1001 Na completely blocked AP and depolarized the RP significantly. These effects were not reversible. As the structure of SC1001 Na is different from that of heterocycloguanidine Na channel blocker, such as TTX, or that of local anesthetics, we infer that SC1001 Na may be a new sodium channel blocker.
Liu
Y
Y
Guo
L
L
Wu
L
L
Geng
Z
Z
Chai
H
H
Xie
Y
Y
D000200:Action Potentials / Q000187:drug effects; D000818:Animals; D002023:Bufo bufo; D008564:Membrane Potentials / Q000187:drug effects; D018485:Muscle Fibers, Skeletal / Q000502:physiology*; D012964:Sodium / Q000494:pharmacology*; D026941:Sodium Channel Blockers
D026941:Sodium Channel Blockers; C072444:SC 1001; D012964:Sodium