Description
A GAT-1 inhibitor (IC50 = 0.04 µM for the human transporter); 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; inhibits GABA uptake in rat synaptosome preparations, neurons, and glia (IC50s = 47, 1,238, and 636 nM, respectively); inhibits PTZ- or DMCM-induced clonic seizures 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 decreases mechanical allodynia and thermal hyperalgesia in a rat model of CCI-induced neuropathic pain at 100 or 200 µg/animal
Formal name: 1-[2-[[(diphenylmethylene)amino]oxy]ethyl]-1,2,5,6-tetrahydro-3-pyridinecarboxylic acid, monohydrochloride
Synonyms: NNC 05-711|NO-711
Molecular weight: 386.9
CAS: 145645-62-1
Purity: ≥98%
Formulation: A crystalline solid
