Pyrazolopyridinones as functionally selective GABA A ligands

2,5-Dihydro-3 H-pyrazolo[4,3- c]pyridin-3-ones are GABA A receptor benzodiazepine binding site ligands, which can exhibit functional selectivity for the α 3 subtype over the α 1 subtype. SAR studies to optimize this functional selectivity are described. 2,5-Dihydro-3 H-pyrazolo[4,3- c]pyridin-3-ones...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 15; no. 22; pp. 4998 - 5002
Main Authors Blackaby, Wesley P., Atack, John R., Bromidge, Frances, Lewis, Richard, Russell, Michael G.N., Smith, Alison, Wafford, Keith, McKernan, Ruth M., Street, Leslie J., Castro, José L.
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 15.11.2005
Subjects
GABA A
Pyrazolopyridinones
GABA A
Pyrazolopyridinones
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Summary:2,5-Dihydro-3 H-pyrazolo[4,3- c]pyridin-3-ones are GABA A receptor benzodiazepine binding site ligands, which can exhibit functional selectivity for the α 3 subtype over the α 1 subtype. SAR studies to optimize this functional selectivity are described. 2,5-Dihydro-3 H-pyrazolo[4,3- c]pyridin-3-ones are GABA A receptor benzodiazepine binding site ligands, which can exhibit functional selectivity for the α 3 subtype over the α 1 subtype. SAR studies to optimize this functional selectivity are described.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.08.006