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General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors.

Abstract：

:Certain spiders contain large pools of polyamine toxins, which are putative pharmacological tools awaiting further discovery. Here we present a general synthesis strategy for this class of toxins and prepare five structurally varied polyamine toxins. Electrophysiological testing at three ionotropic glutamate receptor subtypes reveals that two of these, Nephila polyamine toxins 1 (NPTX-1) and 8 (NPTX-8), comprise intriguing pharmacological activities by having subnanomolar IC(50) values at kainate receptors.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Lucas S,Poulsen MH,Nørager NG,Barslund AF,Bach TB,Kristensen AS,Strømgaard K

doi

10.1021/jm301255m

subject

Has Abstract

pub_date

2012-11-26 00:00:00

pages

10297-301

issue

22

eissn

0022-2623

issn

1520-4804

journal_volume

55

pub_type

杂志文章

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