CNS-5161 hydrochloride (CNS 5161A) (Synonyms: CNS 5161A) |
| Katalog-Nr.GC32553 |
CNS-5161-Hydrochlorid (CNS 5161A) ist ein neuartiger NMDA-Ionenkanalantagonist, der mit der NMDA-Rezeptor-/Ionenkanalstelle interagiert, um eine nicht-kompetitive Blockade der Wirkung von Glutamat zu erzeugen.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 160756-38-7
Sample solution is provided at 25 µL, 10mM.
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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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