A Synthetic Approach to Develop Peptide Inhibitors Selective for Brain-Type Sodium Channels on the Basis of Pompilidotoxin Structure

Hitoshi Nakayama, Sawana Yokote, Ritsuko Setoguchi,Eisuke Shimizu,Kohichi Kawahara,Akihiko Kuniyasu,Tetsuya Shirasaki,Kazuo Takahama,Nobufumi Kawai,Kaoru Yamaoka,Eiji Kinoshita

HETEROCYCLES（2009）

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摘要

To develop inhibitors that are selective for brain-type sodium channels, several peptides were synthesized on the basis of pompilidotoxin structure. A peptide having N-terminal 7 amino acids and its homologs in which Phe(7) is substituted into more hydrophobic amino acids, selectively inhibit sodium current of brain-type sodium channels.

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关键词

Pompilidotoxin Analog,Peptide Inhibitor,Brain-Type Sodium Channel,Brain Ischemia,Whole-Cell Clamp

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