Abstract
2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones are GABAA receptor benzodiazepine binding site ligands with functional selectivity for the alpha3 subtype over the alpha1 subtype. SAR studies to optimise this functional selectivity are described.
MeSH terms
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Animals
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Benzodiazepines / chemistry
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Benzodiazepines / metabolism
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Binding Sites
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Humans
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Kinetics
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Ligands
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Molecular Structure
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Patch-Clamp Techniques
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Pyrazoles / chemical synthesis*
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Pyrazoles / pharmacology
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Pyridines / chemistry
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Pyridines / metabolism
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Radioligand Assay
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Receptors, GABA-A / metabolism*
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Structure-Activity Relationship
Substances
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Ligands
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Pyrazoles
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Pyridines
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Receptors, GABA-A
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CGS 17867A
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Benzodiazepines