AZD7325 是具有口服活性的α2和α3受体正向别构调节剂,Ki分别是 0.3 和 1.3 nM。它是中等CYP1A2和强效CYP3A4诱导剂,有用于焦虑和 dravet 综合征相关的研究潜力。
半岛bd体育手机客户端 描述
AZD-7325 is a GABA-Aα2,3 -selective receptor modulator.
体内活性
AZD7325 on synaptic responses was more prominent in mice on the 129S6/SvEvTac background strain that has been demonstrated to be seizure resistant in the model of Dravet syndrome (Scn1a+/?) and in which the α2 GABAA receptor subunits are higher relative to in the C57BL/6J strain.?Consistent with this, treatment of mice with AZD7325 is associated with a higher temperature threshold for hyperthermia-induced seizures in Scn1a+/? mice without apparent sedative effects.?Our results in a model system indicate that selective targeting α2 is a potential therapeutic option for Dravet syndrome[1].
动物实验
Animal Model:Male and female P18 - P20 F1.Scn1a+/- mice. Dosage:10, 17.8 or 31.6 mg/kg. Administration:Oral administration[1]
Cas No.
942437-37-8
分子式
C19H19FN4O2
分子量
354.385
别名
AZD-7325
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years