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.
Blackaby
Wesley P
WP
Neuroscience Research Centre, Merck Sharp & Dohme Research Laboratories, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. Wesley_Blackaby@Merck.com
Atack
John R
JR
Bromidge
Frances
F
Lewis
Richard
R
Russell
Michael G N
MG
Smith
Alison
A
Wafford
Keith
K
McKernan
Ruth M
RM
Street
Leslie J
LJ
Castro
José L
JL
D001391:Azo Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D008024:Ligands; D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*; D011963:Receptors, GABA-A / Q000378:metabolism*; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D001391:Azo Compounds; D008024:Ligands; D011725:Pyridines; D011963:Receptors, GABA-A; C023666:pyridine