A Pyridazine Series of α2/α3 Subtype Selective GABAA Agonists for the Treatment of Anxiety
RT Lewis, WP Blackaby, T Blackburn… - Journal of medicinal …, 2006 - ACS Publications
RT Lewis, WP Blackaby, T Blackburn, ASR Jennings, A Pike, RA Wilson, DJ Hallett…
Journal of medicinal chemistry, 2006•ACS PublicationsThe development of a series of GABAA α2/α3 subtype selective pyridazine based
benzodiazepine site agonists as anxiolytic agents with reduced sedative/ataxic potential is
described, including the discovery of 16, a remarkably α3-selective compound ideal for in
vivo study. These ligands are antagonists at the α1 subtype, with good CNS penetration and
receptor occupancy, and excellent oral bioavailability.
benzodiazepine site agonists as anxiolytic agents with reduced sedative/ataxic potential is
described, including the discovery of 16, a remarkably α3-selective compound ideal for in
vivo study. These ligands are antagonists at the α1 subtype, with good CNS penetration and
receptor occupancy, and excellent oral bioavailability.
The development of a series of GABAA α2/α3 subtype selective pyridazine based benzodiazepine site agonists as anxiolytic agents with reduced sedative/ataxic potential is described, including the discovery of 16, a remarkably α3-selective compound ideal for in vivo study. These ligands are antagonists at the α1 subtype, with good CNS penetration and receptor occupancy, and excellent oral bioavailability.
ACS Publications