Abstract
Several N-(2-methyl or 1,2-dimethylindol-3-ylglyoxylyl)amino acid derivatives were synthesized and tested for their affinity for the benzodiazepine receptor in bovine cortical membranes. The 2-methyl derivatives showed a lower affinity than the unmethylated analogues, and the 1,2-dimethyl derivatives practically lacked any affinity for the benzodiazepine receptor. The importance of the indole N-H group is therefore evidenced for an optimal interaction of these ligands with receptor site.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acids / chemical synthesis*
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Amino Acids / pharmacology
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Animals
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Binding, Competitive / drug effects
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Cattle
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Cerebral Cortex / drug effects
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Cerebral Cortex / metabolism
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Chemical Phenomena
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Chemistry
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Flunitrazepam / metabolism
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Glyoxylates / chemical synthesis
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Glyoxylates / pharmacology
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In Vitro Techniques
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Indoles / chemical synthesis*
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Indoles / pharmacology
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Magnetic Resonance Spectroscopy
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Membranes / drug effects
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Membranes / metabolism
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Receptors, GABA-A / drug effects*
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Receptors, GABA-A / metabolism
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Spectrophotometry, Infrared
Substances
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Amino Acids
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Glyoxylates
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Indoles
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Receptors, GABA-A
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Flunitrazepam