Abstract
Screening of the Roche compound depository led to the identification of (1-benzyloxy-4,5-dihydro-1H-imidazol-2-yl)-butyl amine 4, a structurally novel NR1/2B subtype selective NMDA receptor antagonist. The structure-activity relationships developed in this series resulted in the discovery of a novel class of potent and selective NMDA receptor blockers displaying activity in vivo.
MeSH terms
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Animals
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Cells, Cultured
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Excitatory Amino Acid Antagonists / administration & dosage
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Excitatory Amino Acid Antagonists / chemistry*
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Excitatory Amino Acid Antagonists / pharmacology
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Imidazoles / administration & dosage
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Imidazoles / chemistry*
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Imidazoles / pharmacology
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Injections, Intraperitoneal
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Mice
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Mice, Inbred DBA
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Potassium Channels, Voltage-Gated / antagonists & inhibitors
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Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
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Receptors, N-Methyl-D-Aspartate / physiology
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Seizures / prevention & control
Substances
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Excitatory Amino Acid Antagonists
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Imidazoles
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NR1 NMDA receptor
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NR2B NMDA receptor
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Potassium Channels, Voltage-Gated
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Receptors, N-Methyl-D-Aspartate