NNC-711

NNC-711 (NO-711 hydrochloride) is a potent and selective inhibitor of GAT-1 (GABA transporter 1) with IC₅₀ values of 0.04, 0.38, 171, 1700, 349, 622 μM for human GAT-1, rat GAT-1, rGAT-2, hGAT-3, rGAT-3, hBGT-3, respectively. NNC-711 has anticonvulsant and analgesic effect in vivo and exhibits cognition-enhancing activity^{[1][2][3][4][5]}. In Vitro:NNC-711 is a potent inhibitor of [³H]GABA uptake in vitro in both rat brain synaptosomes (IC₅₀ = 47 nM), and neuronal (IC₅₀ = 1238 nM) and glial (IC₅₀ = 636 nM) elements^[4].
NNC-711 displaces [³H]tiagabine binding from the GABA uptake carrier in vitro (IC₅₀ = 20 nM)^[4].
NNC-711 (1 μM, 0-15 min) significantly reduces Na⁺-dependent GABA uptake in microglial cell^[5].
In Vivo:NNC-711 (0.25-3 mg/kg; i.p.; 30 min prior to training) prevents amnesia for a passive avoidance task induced by the acetylcholine receptor antagonist Scopolamine (HY-N0296) in male Wistar rat^[2].
NNC-711 (0.5-3 mg/kg; i.p.; immediately prior to occlusion) protects against ischemia-induced death of CA1 pyramidal neurons in a model of bilateral common carotid artery occlusion in the gerbil^[2].
NNC-711 (0.5-1.5 mg/kg; i.p.; immediately prior to training) exhibits significant cognition-enhancing actions in postnatal day 80 male and 28-month old female Wistar rats^[2].
NNC-711 (NO-711) (50-200 μg/10 μL; i.t.; once) effectively develops analgesic effect in sciatic nerve CCI rats modelc^[3].
NNC-711 (0.3-30 mg/kg, i.p.; 30 min before testing) exhibits anticonvulsant effects in Multiple mices and rats epilepsy model^[4].