Back to Search
Start Over
A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2006 Apr 20; Vol. 49 (8), pp. 2600-10. - Publication Year :
- 2006
-
Abstract
- The development of a series of GABA(A) alpha2/alpha3 subtype selective pyridazine based benzodiazepine site agonists as anxiolytic agents with reduced sedative/ataxic potential is described, including the discovery of 16, a remarkably alpha3-selective compound ideal for in vivo study. These ligands are antagonists at the alpha1 subtype, with good CNS penetration and receptor occupancy, and excellent oral bioavailability.
- Subjects :
- Animals
Anti-Anxiety Agents administration & dosage
Anti-Anxiety Agents chemical synthesis
Binding Sites
GABA Agonists administration & dosage
GABA Agonists chemical synthesis
Humans
Ligands
Molecular Structure
Pyridazines administration & dosage
Pyridazines chemical synthesis
Rats
Recombinant Proteins agonists
Stereoisomerism
Structure-Activity Relationship
Anti-Anxiety Agents pharmacology
Anxiety drug therapy
GABA Agonists pharmacology
GABA-A Receptor Agonists
Pyridazines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0022-2623
- Volume :
- 49
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 16610803
- Full Text :
- https://doi.org/10.1021/jm051144x