Abstract
2-(9-Xanthylmethyl)-2-(2'-carboxycyclopropyl) glycine 6e is a novel metabotropic glutamate receptor antagonist. A series of alpha, C-3' disubstituted (carboxycyclopropyl)glycines 6f-n were prepared. Antagonist activity was observed for all these compounds at group 2 and group 3 mGluRs. Although they were slightly less active on group 2 mGluRs than non C-3' substituted 6e, the compounds 6f-n were more selective with lesser or no activity on group 1 mGluR subtypes (IC50 values greater than 100 microns).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Cell Line
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Cyclopropanes / chemistry
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Cyclopropanes / pharmacology
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Excitatory Amino Acid Antagonists / chemical synthesis*
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Excitatory Amino Acid Antagonists / pharmacology
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Glycine / analogs & derivatives*
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Glycine / chemistry
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Glycine / pharmacology
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Humans
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Inhibitory Concentration 50
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Neurons / drug effects
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Prosencephalon / drug effects
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Rats
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Receptors, Glutamate / drug effects*
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Structure-Activity Relationship
Substances
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Cyclopropanes
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Excitatory Amino Acid Antagonists
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Receptors, Glutamate
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Glycine