NNC 711 is a potent and selective inhibitor of GABA uptake by GABA T-1( (IC50 values are 0.04, 171, 1700 and 622 μM for hGABA T-1, rGABA T-2, hGABA T-3 and hBGT-1 respectively). GABA transporters belong to the solute carrier family 6 (SLC6) and are sodium- and chloride-dependent members that mediate the rapid removal of GABA. NNC 711 also exhibits cognition-enhancing activity.

A potent and selective inhibitor of GABA T-1

≥99%

Desiccate at 4° C

Solid

NO-711 hydrochloride; 1,2,5,6-Tetrahydro-1-[2-[[(diphenylmethylene)amino]oxy] ethyl]-3-pyridinecarboxylic acid hydrochloride

204-206° C

541.2° C at 760 mmHg (Predicted)

HGAT-1: IC50 = 0.04 μM ; RGAT-2: IC50 = 171 μM ; HGAT-3 : IC50 = 1700 μM ; HBGT-1: IC50 = 622 μM

pKa: 3.56 (Predicted), pKb: 7.76 (Predicted)

GABA transporter 1: Ki= 47 nM (Rattus norvegicus)

Soluble in water (≥10 mg/mL) at 60° C, ethanol (10 mM), and DMSO (100 mM).

MFCD00153853

123738