NS11394

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、亚型选择性的、口服的 GABAA 受体正调节剂。

A potent, subtype-selective, orally available GABAA receptor positive modulator with Ki of 0.4, 0.8, 0.5 and 0.1 nM for α1, α2, α3 and α5 subunits together with β3γ2; displays 600 to 2000-fold over GABAA-α4 or GABAA-α6 containing receptors; exhibits in vivo anxiolytic efficacy, attenuates spontaneous nociceptive behaviors in response to hindpaw injection of formalin and capsaicin in rats.

——

NS11394 (1-120 mg/kg) selectively attenuates injury-induced nociceptive behaviors in the formalin test.NS11394 (1–10 mg/kg) markedly attenuates the deficit in hindpaw weight bearing [F(4,61) = 7.569, p < 0.001] in CFA rats. Animal Model:Adult male Sprague-Dawley rats.Dosage:1-120 mg/kg.Administration:Orally.Result:Significantly attenuated motor function compared with corresponding vehicle responses.Significantly reduced flinching behavior during interphase [F(3,30) = 4.139, p < 0.05] and the second phase [F(3,30) =11.033, p < 0.001] of the formalin test compared with vehicle treatment indicative of a selective effect on injury-induced nociceptive transmission.

NS-11394

Membrane Transporter/Ion Channel

GAT

GABAA

Neurological Disease

——

951650-22-9

353.4165

C23H19N3O

>98% (HPLC)

DMSO: ≥ 43 mg/mL

N#CC1=CC=CC=C1C2=CC=CC(N3C4=CC=C(C(C)(O)C)C=C4N=C3)=C2

[1,1'-Biphenyl]-2-carbonitrile, 3'-[5-(1-hydroxy-1-methylethyl)-1H-benzimidazol-1-yl]-

(-20℃)

With Ice Pack

≥ 2 years