Α5IA

Chemical compound From Wikipedia, the free encyclopedia

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.[1][2]

Other namesLS-193,268
ATC code
  • None
Quick facts Clinical data, Other names ...
α5IA
Clinical data
Other namesLS-193,268
ATC code
  • None
Pharmacokinetic data
Elimination half-life2-2.5h
Identifiers
  • 3-(5-methylisoxazol-3-yl)-6-[(1-methyl-1H-1,2,3-triazol-4-yl)methoxy][1,2,4]triazolo[3,4-a]phthalazine
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC17H14N8O2
Molar mass362.353 g·mol−1
3D model (JSmol)
  • CC1=CC(=NO1)C2=NN=C3N2N=C(C4=CC=CC=C43)OCC5=CN(N=N5)C
  • InChI=1S/C17H14N8O2/c1-10-7-14(22-27-10)16-20-19-15-12-5-3-4-6-13(12)17(21-25(15)16)26-9-11-8-24(2)23-18-11/h3-8H,9H2,1-2H3
  • Key:NZMJFRXKGUCYNP-UHFFFAOYSA-N
Close

Clinical research

Administration of α5IA following alcohol consumption was found to reverse memory impairments induced by alcohol.[3]

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).[4]

See also

References

Related Articles

Wikiwand AI