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NNC 05-2090 is an antagonist of betaine/GABA transporter 1 (BGT1; IC50 = 5.1 µM for the human transporter).1 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 = 29.62, 45.29, 22.51, 5.29, 7.91, and 4.08 µM, respectively, in CHO cells expressing the mouse or rat transporters).2 Intravenous administration of NNC 05-2090 (0.01 or 0.03 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).3
WARNING This product is not for human or veterinary use.
1. Cyclopropane-
2. Antiallodynic action of 1-
3. Anticonvulsant properties of two GABA uptake inhibitors NNC 05-