A Pyridazine Series of α2/α3 Subtype Selective GABAA Agonists for the Treatment of Anxiety
- 22 March 2006
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 49 (8) , 2600-2610
- https://doi.org/10.1021/jm051144x
Abstract
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.Keywords
This publication has 6 references indexed in Scilit:
- A New Pyridazine Series of GABAA α5 LigandsJournal of Medicinal Chemistry, 2005
- An Orally Bioavailable, Functionally Selective Inverse Agonist at the Benzodiazepine Site of GABAA α5 Receptors with Cognition Enhancing PropertiesJournal of Medicinal Chemistry, 2004
- Analysis of the Set of GABAA Receptor Genes in the Human GenomeJournal of Biological Chemistry, 2004
- Palladium-Catalyzed Coupling Reactions of Aryl ChloridesAngewandte Chemie International Edition in English, 2002
- Synthesis of arylboronates via the palladium(0)-catalyzed cross-coupling reaction of tetra(alkoxo)diborons with aryl triflatesTetrahedron Letters, 1997
- Halogenation Using N-Halogenocompounds. II. Acid Catalyzed Bromination of Aromatic Compounds with 1,3-Dibromo-5,5-dimethylhydantoinBulletin of the Chemical Society of Japan, 1994