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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Excitatory Amino Acid Antagonists / chemical synthesis*
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Excitatory Amino Acid Antagonists / chemistry
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Excitatory Amino Acid Antagonists / pharmacology*
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Indoleacetic Acids
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Phenylacetates / chemical synthesis*
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Phenylacetates / chemistry
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Phenylacetates / pharmacology*
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Polyamines / chemical synthesis*
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Polyamines / chemistry
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Polyamines / pharmacology*
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Protein Conformation
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Receptors, AMPA / antagonists & inhibitors*
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Receptors, AMPA / chemistry
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Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
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Receptors, N-Methyl-D-Aspartate / chemistry
Substances
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Excitatory Amino Acid Antagonists
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Indoleacetic Acids
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Phenylacetates
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Polyamines
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Receptors, AMPA
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Receptors, N-Methyl-D-Aspartate
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argiotoxin-636