NNC-711 (hydro<wbr/>chloride)

NNC-711 (hydrochloride)

CAT N°: 29687
Price:

From 48.00 40.80

NNC-711 is an inhibitor of GABA transporter 1 (GAT-1; IC50 = 0.04 µM for the human transporter).{46780} It is selective for GAT-1 over human GAT-3 and BGT-3 (IC50s = 1,700 and 622 µM, respectively), rat GAT-2 (IC50 = 171 µM), and a panel of 21 receptors and ion channels (IC50s = >50 µM for all) in radioligand binding assays.{46780,46781} NNC-711 inhibits GABA uptake in rat synaptosome preparations, neurons, and glia (IC50s = 47, 1,238, and 636 nM, respectively).{46781} In vivo, NNC-711 inhibits clonic seizures induced by pentylenetetrazole (PTZ; Item No. 18682) or DMCM in mice (ED50s = 1.2 and 3 mg/kg, respectively), as well as audiogenic tonic seizures in mice (ED50 = 0.23 mg/kg) and PTZ-induced tonic seizures in rats (ED50 = 1.7 mg/kg). Intrathecal administration of NNC-711 (100 or 200 µg/animal) decreases mechanical allodynia and thermal hyperalgesia in a rat model of neuropathic pain induced by chronic constriction injury (CCI).{46782}

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