Premium
Synthesis and Biological Activity of Argiotoxin 636 and Analogues: Selective Antagonists for Ionotropic Glutamate Receptors
Author(s) -
Nelson Jared K.,
Frølund Sidsel U.,
Tikhonov Dennis B.,
Kristensen Anders S.,
Strømgaard Kristian
Publication year - 2009
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200805426
Subject(s) - ionotropic effect , polyamine , glutamate receptor , chemistry , ion channel , receptor , pharmacology , kainate receptor , stereochemistry , amine gas treating , biochemistry , biology , ampa receptor , organic chemistry
Abstract More discerning than the parent : Analogues of the polyamine toxin argiotoxin 636 (shown docked in the ion channel of an ionotropic glutamate (iGlu) receptor; N blue, O red) distinguish subtypes of iGlu receptors. Depending on which of the two internal amine groups is replaced with a methylene group, the analogue inhibits one or other of two receptor subtypes as potently as the natural compound, which itself inhibits both subtypes nonselectively.