NNC 05-2090 (hydrochloride)

NNC 05-2090 is an antagonist of betaine/GABA transporter 1 (BGT1, IC50 = 5. µM for the human transporter). It also inhibits mouse GABA transporter 1 (GAT1), mouse GAT2, mouse GAT3, rat serotonin transporter (SERT), rat noradrenaline transporter (NET), and rat dopamine transporter (DAT, IC50s = 29. 45. 22. 5. 7. and 4. µM, respectively, in CHO cells expressing the mouse or rat transporters). Intravenous administration of NNC 05-2090 (0. or 0. mg/kg) increases the latency to paw withdrawal in a mouse model of partial sciatic nerve ligation-induced allodynia. It decreases immobility time in the forced swim test in mice when administered at a dose of 2 mg/kg. NNC 05-2090 inhibits sound-induced clonic and tonic seizures and maximal electroshock-induced seizures in mice (ED50s = 26, 19, and 73 µmol/kg, respectively).. Solulibility: Acetonitrile: Slightly Soluble: 0.1-1 mg/ml: DMSO: Slightly Soluble: 0.1-1 mg/ml, Water: Slightly Soluble: 0.1-1 mg/ml.