CNS-5161 hydrochloride 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。
半岛bd体育手机客户端
描述
CNS-5161 hydrochloride is a new antagonist of NMDA ion-channel. It interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
体外活性
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.
体内活性
In the neonatal rat NMDA excitotoxicity model in vivo, CNS-5161 (i.p.) protects against the necrotic effects of exogenous N-methyl-D-aspartate (ED80: 4 mg/kg). 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 hypoxic/ischaemic brain injury in neonatal rats[1].
Cas No.
160756-38-7
分子式
C16H19Cl2N3S2
分子量
388.38
别名
CNS 5161A
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years