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NS 11394
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NS 11394图片
CAS NO:951650-22-9
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
NS 11394 是一种具有口服活性且独特的亚型选择性 GABAA 阳性变构受体 (PAM),Ki 约为 0.5 nM。
Cas No.951650-22-9
别名3'-[5-(1-羟基-1-甲基乙基)-1H-苯并咪唑-1-基]-[1,1'-联苯]-2-甲腈
化学名3'-(5-(2-hydroxypropan-2-yl)-1H-benzo[d]imidazol-1-yl)-[1,1'-biphenyl]-2-carbonitrile
Canonical SMILESCC(C1=CC(N=CN2C3=CC=CC(C4=CC=CC=C4C#N)=C3)=C2C=C1)(O)C
分子式C23H19N3O
分子量353.42
溶解度≥ 35.3mg/mL in DMSO with gentle warming
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

NS 11394 is a selective GABA(A) receptor-positive modulator.

Preclinical studies suggest that GABAA-1, 2, and 5-containing receptors can mediate the sedative/ motor-impairing, anxiolytic, and memory impairing effects, respectively.

In vitro: Previous study showed that NS11394 possessed a functional selectivity profile at GABA(A) receptors of alpha(5) >alpha(3) >alpha(2) >alpha(1) based on oocyte electrophysiology with human GABA(A) receptors. Moreover, compared with other subtype-selective ligands, NS11394 was unique in having superior efficacy for GABA(A)-alpha(3) receptors while maintaining low efficacy for GABA(A)-alpha(1) receptors [1].

In vivo: Animal study showed that NS11394 had an excellent PK profile, which correlated with pharmacodynamic endpoints of CNS receptor occupancy. In addition, it was showd that NS11394 was potent and highly effective in rodent anxiety models. The anxiolytic efficacy of NS11394 was most probably mediated via its high efficacy at GABA(A)-alpha(3) receptors, though the contribution of GABA(A)-alpha(2) receptors could not be excluded. Moreover, when compared with benzodiazepines, NS11394 had a significantly reduced side effect profile in rat and mouse, even at full CNS receptor occupancy. The authors attributed such benign side effect profile to very low efficacy of NS11394 at GABA(A)-alpha(1) receptors and a partial agonist profile of receptor subtypes. It was also found that NS11394 could impair memory in both rats and mice, which was possibly attributable to its efficacy at GABA(A)-alpha(5) receptors [1].

Clinical trial: Up to now, NS 11394 is still in the preclinical development stage.

Reference:
[1] Mirza NR, et al.  NS11394 [3'-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl- 2-carbonitrile], a unique subtype-selective GABAA receptor positive allosteric modulator: in vitro actions, pharmacokinetic properties and in vivo anxiolytic efficacy. J Pharmacol Exp Ther. 2008 Dec;327(3):954-68.