Abstract
Imidazo[1,2-a]pyrimidines and imidazo[1,2-b][1,2,4]triazines are ligands for the benzodiazepine binding site of GABA(A) receptors that are functionally selective for the alpha2/alpha3 subtypes over the alpha1 subtype. SAR studies to optimise this functional selectivity, pharmacokinetic and behavioural data are described.
MeSH terms
-
Administration, Oral
-
Animals
-
Anxiety Disorders / drug therapy*
-
Ataxia / drug therapy
-
Binding Sites
-
Biological Availability
-
Disease Models, Animal
-
Dogs
-
Female
-
GABA Agonists / pharmacokinetics
-
GABA Agonists / pharmacology
-
GABA-A Receptor Agonists*
-
Imidazoles / pharmacokinetics
-
Imidazoles / pharmacology*
-
Male
-
Maze Learning / drug effects
-
Molecular Structure
-
Protein Subunits / agonists*
-
Protein Subunits / metabolism
-
Rats
-
Rats, Sprague-Dawley
-
Receptors, GABA-A / metabolism
-
Saimiri
-
Structure-Activity Relationship
-
Triazines / pharmacokinetics
-
Triazines / pharmacology*
Substances
-
GABA Agonists
-
GABA-A Receptor Agonists
-
Gabra2 protein, mouse
-
Gabra3 protein, mouse
-
Imidazoles
-
Protein Subunits
-
Receptors, GABA-A
-
Triazines