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Novel modulator of Na(V)1.1 and Na(V)1.2 Na channels in rat neuronal cells.


ABSTRACT: A novel modulator of sodium ion currents was synthesized in 6 steps from a protected dihydroxypyrrolidine nitrone, via 1,3-dipolar cycloaddition reaction with acrylamide. Sodium ion currents in B50 cells were evaluated in comparison to saxitoxin and tetrodotoxin, and revealed an IC(50) of 15.7 muM. The new compound shows no evidence of binding to the C-lobe of the saxitoxin-binding protein saxiphilin.

SUBMITTER: Mao H 

PROVIDER: S-EPMC2894714 | biostudies-literature | 2010 Mar

REPOSITORIES: biostudies-literature

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Novel modulator of Na(V)1.1 and Na(V)1.2 Na channels in rat neuronal cells.

Mao Hua H   Fieber Lynne A LA   Gawley Robert E RE  

ACS medicinal chemistry letters 20100301 3


A novel modulator of sodium ion currents was synthesized in 6 steps from a protected dihydroxypyrrolidine nitrone, via 1,3-dipolar cycloaddition reaction with acrylamide. Sodium ion currents in B50 cells were evaluated in comparison to saxitoxin and tetrodotoxin, and revealed an IC(50) of 15.7 muM. The new compound shows no evidence of binding to the C-lobe of the saxitoxin-binding protein saxiphilin. ...[more]

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