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CAS No.: 942437-37-8

AZD7325 Catalog No. CSN25262

Synonyms: BAER-101;3-CinnolinecarboxaMide

AZD-7325 is a GABA-Aα2,3 selective receptor modulator.

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靶点选择性

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实验方案

技术信息

生物活性

描述AZD7325 is an α_2,3-subtype-selective GABA-A-receptor modulator. It shows much higher binding affinity at the α_2,3-subunits (K_i = 0.3nM and 1.3nM, respectively) over the α₅-subunit (K_i = 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 α_2,3-subunits, neutral antagonism at the α₁ subunit, and weak affinity for the α₅ subunit^[1].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8218 mL
- 14.1092 mL
- 28.2184 mL
- 5 mM
- 0.5644 mL
- 2.8218 mL
- 5.6437 mL
- 10 mM
- 0.2822 mL
- 1.4109 mL
- 2.8218 mL

技术信息

CAS号

942437-37-8

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H19FN4O2

运输

蓝冰

分子量

354.38

别名

BAER-101;3-CinnolinecarboxaMide

溶解度

DMSO	240.0 mg/mL (677.2 mM) warming

动物实验配方

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AZD7325 Catalog No. CSN25262

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