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CNS-5161 hydrochloride(CNS 5161A)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CNS-5161 hydrochloride(CNS 5161A)图片
CAS NO:160756-38-7
规格:98%
分子量:388.38
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
CNS-5161hydrochloride是一种新型NMDA离子通道拮抗剂,与NMDA受体/离子通道位点相互作用,产生对谷氨酸作用的非竞争性阻断。
CAS:160756-38-7
分子式:C16H19Cl2N3S2
分子量:388.38
纯度:98%
存储:Store at -20°C

Background:

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.