AZD-6280

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Chemical Structure| 942436-93-3 同义名 : -
CAS号 : 942436-93-3
货号 : A1177361
分子式 : C20H22N4O3
纯度 : 99%
分子量 : 366.41
MDL号 : MFCD21337368
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 Gamma aminobutyric acid (GABA), a naturally occurring amino acid, is the major inhibitory neurotransmitter in the cerebellum. AZD6280 is an α2/α3 subunit-selective GABAA receptor modulator with Ki values of 21 ± 5nM and 31 ± 17nM for α2 and α3, respectively. It also shows binding affinity to the α1 and α5 subunit with Ki values of 0.5 ± 0.2nM and 1680 ± 650nM, respectively. The in vitro efficacy of AZD6280 at α2 and α3 (32% and 34%, respectively) is 4- to 5-fold higher than that at α1 and α5 (8% and 7%, respectively)[1]. In primary mouse cortical neurons depleted with Disrupted-in-Schizophrenia-1 (DISC1), treatment with 0.1µM AZD6280 for 7 days rescued DISC1 knockdown-induced dendritic abnormalities[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.65mL

2.73mL

1.36mL

27.29mL

5.46mL

2.73mL
参考文献

[1]Chen X, Jacobs G, de Kam ML, et al. AZD6280, a novel partial γ-aminobutyric acid A receptor modulator, demonstrates a pharmacodynamically selective effect profile in healthy male volunteers. J Clin Psychopharmacol. 2015;35(1):22-33.

[2]Saito A, Taniguchi Y, Rannals MD, et al. Early postnatal GABAA receptor modulation reverses deficits in neuronal maturation in a conditional neurodevelopmental mouse model of DISC1. Mol Psychiatry. 2016;21(10):1449-1459.