Bioactivity | CNS-5161 is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate. |
Target | NMDA receptor/ion channel |
Invitro | CNS-5161 (CNS 5161) is a novel and selective noncompetitive antagonist of the NMDA subset of glutamate receptors in the mammalian brain. CNS-5161 has potent inhibitory activity in vitro at the NMDA ion channel and is able to displace [3H] MK-801 binding with a Ki of 1.8 nM in synaptosomal membrane preparations from rat brain[1]. |
In Vivo | In the neonatal rat NMDA excitotoxicity model in vivo, CNS-5161 (CNS 5161) protects against the necrotic effects of exogenous N-methyl-D-aspartate with an ED80 of 4 mg/kg by the intraperitoneal (i.p.) route. CNS-5161 also shows a 91% inhibition of audiogenic seizures in DBA/2 mice at 4 mg/kg i.p., and has a neuroprotective effect following hypoxix/ischaemic brain injury in neonatal rats[1]. |
Name | CNS 5161 |
CAS | 160754-76-7 |
Formula | C16H18ClN3S2 |
Molar Mass | 351.92 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Walters MR, et al. Early clinical experience with the novel NMDA receptor antagonist CNS 5161. Br J Clin Pharmacol. 2002 Mar;53(3):305-11. |