Pyrazolopyridinones as functionally selective GABAA ligands

2,5-Dihydro-3H-pyrazolo[4,3-c]pyridin-3-ones are GABAA receptor benzodiazepine binding site ligands, which can exhibit functional selectivity for the alpha3 subtype over the alpha1 subtype. SAR studies to optimize this functional selectivity are described.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-11, Vol.15 (22), p.4998-5002
Hauptverfasser:	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:	Artikel
Sprache:	eng
Schlagworte:	Azo Compounds - chemical synthesis Azo Compounds - chemistry Azo Compounds - metabolism Biological and medical sciences Gabaergic and benzodiazepinic system Ligands Medical sciences Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Pyridines - chemical synthesis Pyridines - chemistry Pyridines - metabolism Receptors, GABA-A - metabolism Sensitivity and Specificity Structure-Activity Relationship Substrate Specificity
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Beschreibung
Zusammenfassung:	2,5-Dihydro-3H-pyrazolo[4,3-c]pyridin-3-ones are GABAA receptor benzodiazepine binding site ligands, which can exhibit functional selectivity for the alpha3 subtype over the alpha1 subtype. SAR studies to optimize this functional selectivity are described.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.08.006