CNS-5161 hydrochloride (CNS 5161A) 是一种新型 NMDA 离子通道拮抗剂，可与 NMDA 受体/离子通道位点相互作用，对谷氨酸的作用产生非竞争性阻断。
CNS-5161 hydrochloride 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.
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 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].
[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.
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