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

NNC-711 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
145645-62-1
Storage:
-20
UN-No:
Non-Hazardous - /

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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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

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