Cayman Pyrrolidine Linoleamide; Purity- Greater Than Or Equal To

NNC-711 is an inhibitor of GABA transporter 1 (GAT-1; IC₅₀ = 0.04 µM for the human transporter). 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.^, NNC-711 inhibits GABA uptake in rat synaptosome preparations, neurons, and glia (IC₅₀s = 47, 1,238, and 636 nM, respectively). In vivo, NNC-711 inhibits clonic seizures induced by pentylenetetrazole (PTZ; Item No. ) 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).

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