Inhibitors?Screening Libraries?ProteinsMedChemExpressCNS 5161Cat. No.:
HY-101809ACAS No.:160754-76-7分子式:C??H??ClN?S?分子量:351.92作用靶点:iGluR
作用通路:Membrane Transporter/Ion Channel; Neuronal Signaling储存方式:Ple
ase store the product under the recommended conditions inthe Cert
ificate of Analysis.BIOLOGICAL ACTIVITY生物活性CNS-5161 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。IC50 & TargetNMDA rece
ptor/ion channel [1]体外研究CNS-5161 (CNS 5161) is a novel and select
ive noncompetitive antagonist of the NMDA subset of glutamaterece
ptors in the mammalian brain. CNS-5161 has potent inhibitory acti
vity in vitro at the NMDA ion channeland is able to displace [3H]
MK-801 binding with a Ki of 1.8 nM in synaptosomal membrane prep
arationsfrom rat brain [1].体内研究In the neonatal rat NMDA excitotox
icity model in vivo, CNS-5161 (CNS 5161) protects against the nec
roticeffects 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 aneuroprotective effect following hypoxix/ischaemic b
rain injury in neonatal rats [1].REFERENCESWalters MR, et al. Ear
ly clinical experience with the novel NMDA receptor antagonist CN
S 5161. Br J Clin Pharmacol. 2002 Mar;53(3):305-11.McePdfHeightCa
ution: Product has not been fully validated for medical applicati
ons.For research use only.1/1MedChemExpress |
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