Novel modulator of Na(V)1.1 and Na(V)1.2 Na channels in rat neuronal cells.
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.
Mao
Hua
H
Department of Chemistry and Biochemistry, University of Arkansas, Fayetteville, AR 72701.
Fieber
Lynne A
LA
Gawley
Robert E
RE