期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 1, 期 3, 页码 135-138出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml100035t
关键词
Nitrone; 1,3-dipolar cycloaddition; saxitoxin (STX); tetrodotoxin (TTX); sodium channel blocker; B50 cells
资金
- Arkansas Biosciences Institute
- National Institutes of Health [RR 5569]
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 850 cells were evaluated in comparison to saxitoxin and tetrodotoxin and revealed an IC50 of 15.7 mu M. The new compound shows no evidence of binding to the C-lobe of the saxitoxin-binding protein saxiphilin.
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