AZD7325,942437-37-8

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AZD7325

CAS No. : 942437-37-8

MCE 国际站：AZD7325

产品活性：AZD7325 是具有口服活性的 α2,3 receptor 的正向别构调节剂 (PAM)，K_i 分别是 0.3 and 1.3 nM，但在 α1 和 α5 受体亚型上效果较差。AZD7325 是一种中等 CYP1A2 和强效 CYP3A4 诱导剂。AZD7325 具有用于焦虑和 dravet 综合征相关研究的潜力。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling  |  Metabolic Enzyme/Protease

作用靶点：GABA Receptor  |  Cytochrome P450

In Vitro: AZD7325 is a high affinity and selective modulator of the GABAA?receptor system, exhibits high binding affinity at GABAAα1,?α2?and?α3?(K_i=0.5, 0.3, and 1.3 nM, respectively), and low at GABAAα5?(K_i=230 nM).
AZD7325 (0-10 μM; 3 consecutive days; once daily) causes a maximal CYP1A2 mRNA expression of 3.2-fold, 2.1-fold, and 2.5-fold in human hepatocytes from donor HH210, HH215, and HH216, respectively.
AZD7325 (0-10 μM; 3 consecutive days; once daily) causes CYP1A2 and CYP3A4 protein expression in human hepatocytes from donor HH210.

In Vivo: 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.

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