AZD7325

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Chemical Structure| 942437-37-8 同义名 : BAER-101
CAS号 : 942437-37-8
货号 : A1219168
分子式 : C19H19FN4O2
纯度 : 99%+
分子量 : 354.38
MDL号 : MFCD21337369
存储条件:

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 AZD7325 is an α2,3-subtype-selective GABA-A-receptor modulator. It shows much higher binding affinity at the α2,3-subunits (Ki = 0.3nM and 1.3nM, respectively) over the α5-subunit (Ki = 230nM) [1]. AZD7325 at a dosage of 31.6mg/kg significantly prolonged the decay time of miniature inhibitory postsynaptic currents (IPSCs) recorded from the CA1 neurons collected from mice on the 129 background strain. AZD7325 treatment also significantly prolonged the decay time of asynchronous IPSCs in the perisomatic synapses in both F1 and 129 strains. AZD7325 at doses of 10, 17.8, and 31.6mg/kg exhibited a significant protective effect against seizure induction in F1.Scn1a+/- mice[2].
作用机制 AZD7325 is allosteric GABA-A-receptor modulator that demonstrates relatively potent positive modulation at the α2,3-subunits, neutral antagonism at the α1 subunit, and weak affinity for the α5 subunit[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.82mL

0.56mL

0.28mL

14.11mL

2.82mL

1.41mL

28.22mL

5.64mL

2.82mL

参考文献

[1]Chen X, Jacobs G, de Kam M, Jaeger J, Lappalainen J, Maruff P, Smith MA, Cross AJ, Cohen A, van Gerven J. The central nervous system effects of the partial GABA-Aα2,3 -selective receptor modulator AZD7325 in comparison with lorazepam in healthy males. Br J Clin Pharmacol. 2014 Dec;78(6):1298-314. doi: 10.1111/bcp.12413

[2]Nomura T, Hawkins NA, Kearney JA, George AL Jr, Contractor A. Potentiating α2 subunit containing perisomatic GABAA receptors protects against seizures in a mouse model of Dravet syndrome. J Physiol. 2019 Aug;597(16):4293-4307. doi: 10.1113/JP277651