Biological Activity
GABA transport inhibitor, showing selectivity for GAT-3 and GAT-2 (IC 50 values are 5, 21 and 388 μ M for hGAT-3, rGAT-2 and hGAT-1 respectively). Increases thalamic GABA levels and is an anticonvulsant following systemic administration in vivo .
References
[1]. borden la, dhar tg, smith ke, et al. cloning of the human homologue of the gaba transporter gat-3 and identification of a novel inhibitor with selectivity for this site. receptors channels, 1994, 2(3): 207-213.
[2]. pabel j, faust m, prehn c, et al. development of an (s)-1-{2-[tris(4-methoxyphenyl)methoxy]ethyl}piperidine-3-carboxylic acid [(s)-snap-5114] carba analogue inhibitor for murine γ-aminobutyric acid transporter type 4. chemmedchem, 2012, 7(7): 1245-1255.
[3]. dalby no. gaba-level increasing and anticonvulsant effects of three different gaba uptake inhibitors. neuropharmacology, 2000, 39(12): 2399-2407.
[4]. kataoka k, hara k, haranishi y, et al. the antinociceptive effect of snap5114, a gamma-aminobutyric acid transporter-3 inhibitor, in rat experimental pain models. anesth analg, 2013, 116(5): 1162-1169.
