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Angew Chem Int Ed Engl. 2009;48(17):3087-91. doi: 10.1002/anie.200805426.

Synthesis and biological activity of argiotoxin 636 and analogues: selective antagonists for ionotropic glutamate receptors.

Author information

1
Department of Medicinal Chemistry, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark.

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.

PMID:
19152392
DOI:
10.1002/anie.200805426
[Indexed for MEDLINE]

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