α₅IA (LS-193,268) is a

nootropic Nootropics ( , or ) (colloquial: smart drugs and cognitive enhancers, similar to adaptogens) are a wide range of natural or synthetic dietary supplement, supplements or drugs and other substances that are claimed to improve cognitive function ...

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 GABA_A

receptor Receptor may refer to: * Sensory receptor, in physiology, any structure which, on receiving environmental stimuli, produces an informative nerve impulse *Receptor (biochemistry), in biochemistry, a protein molecule that receives and responds to a ...

. It binds to the α₁, α₂, α₃ and α₅ subtypes.

In Vivo Electrophysiology

Recordings of

local field potentials Local field potentials (LFP) are transient electrical signals generated in nervous and other tissues by the summed and synchronous electrical activity of the individual cells (e.g. neurons) in that tissue. LFP are "extracellular" signals, meaning ...

indicate that oral administration of α5IA increases the amplitude of sharp wave ripples which are implicated in memory function in adult wild type rats. It is intriguing to note that 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).

References

{{DEFAULTSORT:A5ia GABAA receptor negative allosteric modulators Isoxazoles Aromatic ethers Phthalazines Triazoles

In Vivo Electrophysiology

See also

References