| Description | CNS-5161 hydrochloride (CNS 5161A) 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. |
| In vitro | CNS-5161在体外对NMDA离子通道表现出强大的抑制活性，并能在大鼠脑突触膜制备中以1.8 nM的Ki值置换[3H] MK-801的结合。 |
| In vivo | 在新生大鼠体内NMDA兴奋毒性模型中，CNS-5161 (i.p.) 可阻断外源性N-甲基-D-天门冬氨酸（ED80：4 mg/kg）引起的坏死效应。CNS-5161在以4 mg/kg i.p.剂量给药时可抑制DBA/2小鼠的音源性癫痫，并在新生大鼠缺氧/缺血性脑损伤后显现出神经保护作用[1]。 |
| Synonyms | CNS 5161A |
| molecular weight | 388.38 |
| Molecular formula | C16H19Cl2N3S2 |
| CAS | 160756-38-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (141.61 mM) |
| References | 1. Walters MR, et al. Early clinical experience with the novel NMDA receptor antagonist CNS 516Br J Clin Pharmacol. 2002 Mar;53(3):305-11. |