2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor.
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.
Mitchinson
Andrew
A
Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow CM20 2QR, UK. andrew_mitchinson@merck.com
Atack
John R
JR
Blurton
Peter
P
Carling
Robert W
RW
Castro
José L
JL
Curley
Karen S
KS
Russell
Michael G N
MG
Marshall
George
G
McKernan
Ruth M
RM
Moore
Kevin W
KW
Narquizian
Robert
R
Smith
Alison
A
Street
Leslie J
LJ
Thompson
Sally-Anne
SA
Wafford
Keith
K
D000818:Animals; D001569:Benzodiazepines / Q000737:chemistry / Q000378:metabolism; D001665:Binding Sites; D006801:Humans; D007700:Kinetics; D008024:Ligands; D015394:Molecular Structure; D018408:Patch-Clamp Techniques; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D011725:Pyridines / Q000737:chemistry / Q000378:metabolism; D011869:Radioligand Assay; D011963:Receptors, GABA-A / Q000378:metabolism*; D013329:Structure-Activity Relationship
D008024:Ligands; D011720:Pyrazoles; D011725:Pyridines; D011963:Receptors, GABA-A; C054730:CGS 17867A; D001569:Benzodiazepines