CNS-5161 hydrochloride  (Synonyms: CNS 5161A)

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.

NMDA receptor/ion channel^[1]

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 K_i of 1.8 nM in synaptosomal membrane preparations from rat brain^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

388.38

C₁₆H₁₉Cl₂N₃S₂

160756-38-7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]