δ-GABAA receptors are emerging as an important pharmacological target. DS1 potently (low nM) enhances GABA-evoked currents mediated by α4β3δ receptors. It had little effect on GABA responses mediated by α4β3γ2 receptors. At similar concentrations DS1 directly activates this receptor and is the most potent known agonist of α4β3δ receptors. This compound has an opportunity to be become an agonist golden stardard for δ-GABAA receptors.
Etomidate is a general anesthetic; potentiates GABAA transmission. The possible neuroprotective effect of etomidate against streptozotocin-induced (STZ-induced) hyperglycaemia were investigated in the rat brain and spinal cord. Etomidate treatment demonstrated neuroprotective effect on the neuronal tissue against the diabetic oxidative damage
α5IA is a selective inverse agonist for a5 subtype of GABAA receptor with a higher intrincing efficacy to the a5 subtype than other drugs. α5IA enhances cognition in laboratory animals without being proconvulsant or anxiogenic-like. More important, α5IA acts as an "alcohol antagonist" markedly reducing the amnestic effect of alcohol and partially attenuating the sedative action. This activity is similar to Ro15-4513, but Ro15-4513 is predicted to cause exiety in human. a5IR offers a possibility to study cognitive disorders, memory function, and treatment of alcohol related disorders.
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