Novel modulator of NaV1.1 and NaV1.2 Na+ channels in rat neuronal cells

Hua Mao, Lynne A. Fieber, Robert E. Gawley

Research output: Contribution to journalArticlepeer-review

10 Scopus citations

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 IC50 of 15.7 μM. The new compound shows no evidence of binding to the C-lobe of the saxitoxin-binding protein saxiphilin.

Original languageEnglish (US)
Pages (from-to)135-138
Number of pages4
JournalACS Medicinal Chemistry Letters
Volume1
Issue number3
DOIs
StatePublished - Jun 10 2010

Keywords

  • 1,3-dipolar cycloaddition
  • B50 cells
  • Nitrone
  • saxitoxin (STX)
  • sodium channel blocker
  • tetrodotoxin (TTX)

ASJC Scopus subject areas

  • Organic Chemistry
  • Drug Discovery
  • Biochemistry

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