L-838,417

L-838,417 is a **nonbenzodiazepine anxiolytic** used in scientific research, with a mechanism and effects similar to benzodiazepines but a distinct structure. It acts as a **subtype-selective positive allosteric modulator of the GABA-A receptor**: specifically, a **partial agonist** at α2, α3, and α5 subunits, and a **negative allosteric modulator** at the α1 subunit, with little affinity for α4 and α6. This results in **anxiolytic effects** predominantly mediated by α2 and α3 subtypes, with minimal sedative or amnestic properties (as those are more related to α1). L-838,4417 has been shown in preclinical models to display non-sedative anxiolytic, antinociceptive (pain-reducing), and anti-inflammatory activity in vivo. It is used exclusively in research settings and is not approved for clinical use, having been developed by Merck, Sharp and Dohme[1][4][5][10].

Other names

7-(tert-butyl)-3-(2,5-difluorophenyl)-6-((1-methyl-1H-1,2,4-triazol-5-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine