• 产品描述： AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.

• 靶点： CYP1A2;CYP3A4;P450; GABAReceptor

• 体内研究：
  AZD7325 (oral administration; 10, 17.8 or 31.6 mg/kg; 30 minutes before the induction of hyperthermia) attenuates hyperthermia-induced seizures, shows median thresholds in the treatment groups of 42.8°C for 10 mg/kg, 43.3°C for 17.8 mg/kg, and 43.4°C for 31.6 mg/kg compares to 42.2°C in vehicle group. Animal Model: Male and female P18 - P20 F1.Scn1a+/- mice Dosage: 10, 17.8 or 31.6 mg/kg Administration: Oral administration; 30 minutes before the induction of hyperthermia Result: Attenuated hyperthermia-induced seizures in F1.Scn1a+/- mice with no sedative effect.

• 参考文献：
  1. Chen X, et al. 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. 2. Zhou D, et al. A clinical study to assess CYP1A2 and CYP3A4 induction by AZD7325, a selective GABA(A) receptor modulator - an in vitro and in vivo comparison.Br J Clin Pharmacol. 2012 Jul;74(1):98-108. 3. Nomura T, et al. 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. 4. AZD7325,Mechanism of action: Gamma-aminobutyric acid receptor A alpha 2 & 3 (GABAAα2,3) positive modulator

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	0 ml	0 ml	0 ml
  5 mM	0 ml	0 ml	0 ml
  10 mM	0 ml	0 ml	0 ml
  50 mM	0 ml	0 ml	0 ml

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• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *