NNC-711 (hydrochloride)

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, Cay-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).Formal Name: 1-[2-[[(diphenylmethylene)amino]oxy]ethyl]-1,2,5,6-tetrahydro-3-pyridinecarboxylic acid, monohydrochloride. CAS Number: 145645-62-1. Synonyms: NNC 05-711, NO-711. Molecular Formula: C21H22N2O3 . HCl. Formula Weight: 386.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble, Water: 10 mM. lambdamax: 258 nm. SMILES: OC(C1=CCCN(CCO/N=C(C2=CC=CC=C2)/C3=CC=CC=C3)C1)=O.Cl. InChi Code: InChI=1S/C21H22N2O3.ClH/c24-21(25)19-12-7-13-23(16-19)14-15-26-22-20(17-8-3-1-4-9-17)18-10-5-2-6-11-18,/h1-6,8-12H,7,13-16H2,(H,24,25),1H. InChi Key: YZYRTEYMUTWJPL-UHFFFAOYSA-N.