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AZD-8529 mesylate {[allProObj[0].p_purity_real_show]}

货号:A1329231 Ambeed 开学季,买赠积分,赢豪礼

AZD-8529 is a a positive allosteric modulator at the mGluR2 receptor. AZD8529 decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys. AZD8529 potentiated agonist-induced activation of mGluR2 in the membrane-binding assay and in primate cortex, hippocampus, and striatum. In monkeys, AZD8529 decreased nicotine self-administration at doses (.3-3 mg/kg) that did not affect food self-administration. AZD8529 also reduced nicotine priming- and cue-induced reinstatement of nicotine seeking after extinction of the drug-reinforced responding. In rats, AZD8529 decreased nicotine-induced accumbens dopamine release. The positive allosteric modulators of metabotropic glutamate receptor 2 should be considered for relapse prevention.

AZD-8529 mesylate 化学结构 CAS号:1314217-69-0
AZD-8529 mesylate 化学结构
CAS号:1314217-69-0
AZD-8529 mesylate 3D分子结构
CAS号:1314217-69-0
AZD-8529 mesylate 化学结构 CAS号:1314217-69-0
AZD-8529 mesylate 3D分子结构 CAS号:1314217-69-0
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AZD-8529 mesylate 纯度/质量文件 产品仅供科研

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AZD-8529 mesylate 生物活性

描述 AZD-8529 mesylate is a potent, highly selective and orally active mGluR2-positive modulator with an EC50 of 285 nM and no positive modulation of mGluR1, 3, 4, 5, 6, 7 and 8 isoforms at high concentration[1].AZD-8529 mesylate enhances the effect of glutamate on mGluR2 with an EC50 of 195 nM[1].At a concentration of 25 μM, AZD-8529 mesylate does not induce an antagonistic response to mGluR[1].

AZD-8529 mesylate 动物研究

Animal study At a dose of 0.3 mg/kg, administered intramuscularly, AZD-8529 mesylate reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys[1].Administered intraperitoneally at a dose of 30 mg/kg, AZD-8529 mesylate reduces nicotine-induced increases in extracellular dopamine in the shell of freely moving rat accumbens[1].

AZD-8529 mesylate 参考文献

[1]Justinova Z, et al. The Novel Metabotropic Glutamate Receptor 2 Positive Allosteric Modulator, AZD8529, Decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys. Biol Psychiatry. 2015 Oct 1;78(7):452-62.

AZD-8529 mesylate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.71mL

0.34mL

0.17mL

8.57mL

1.71mL

0.86mL

17.14mL

3.43mL

1.71mL

AZD-8529 mesylate 技术信息

CAS号1314217-69-0
分子式C25H28F3N5O6S
分子量 583.58
别名
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 40 mg/mL(68.54 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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