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Α5IA
α5IA (LS-193,268) is a nootropic drug invented in 2004 by a team working for Merck, Sharp and Dohme, which acts as a subtype-selective inverse agonist at the benzodiazepine binding site on the GABAA receptor. It binds to α1, α2, α3 and α5 -containing subtypes, with functional selectivity for α5-containing subtypes.
Clinical research
Administration of α5IA following alcohol consumption was found to reverse memory impairments induced by alcohol.
In vitro electrophysiology
Recordings of local field potentials indicate that oral administration of α5IA increases the amplitude of sharp wave ripples which are implicated in memory function in adult wild type rats. The increase in ripple amplitude is not seen in adult male TgF344-AD rats which express human β-amyloid precursor protein (with the Swedish mutation) and human presenilin-1 (with a Δ exon 9 mutation).
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