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.
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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]. |
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]. |
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 |
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 |