AZD7325 (Synonyms: BAER-101) |
| رقم الكتالوجGC39342 |
AZD7325 هو PAM انتقائي جزئي فعال وفعال عن طريق الفم لمستقبلات GABAAα2 و Aα3 (Ki = 0.3 و 1.3 نانومتر ، على التوالي) ، وله فعالية معادية أقل في الأنواع الفرعية لمستقبلات Aα1 و Aα5
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Cas No.: 942437-37-8
Sample solution is provided at 25 µL, 10mM.
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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[1][4]. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro[2]. AZD7325 has the potential for the investigation of anxiety and dravet syndrome[3]. PAM: positive allosteric modulator.
[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
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