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  • AZD-8529
AZD-8529的可视化放大

AZD-8529

AZD-8529是一种有效的,高度选择性的,可口服的mGluR2正向调节剂,EC50值为285nM;在20-25M的浓度范围内,对mGluR1,3,4,5,6,7和8没有正向调节作用。

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AZD-8529的二维码
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  • 货号: ajcx12486
  • CAS: 1092453-15-0
  • 别名:
  • 分子式: C24H24F3N5O3
  • 分子量: 487.47
  • 纯度: >98%
  • 溶解度: DMSO: 62.5 mg/mL (128.21 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.


AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes. AZD8529 potentiates the effects of glutamate at mGluR2 with an EC50 of 195±62 nM[1].


AZD-8529 (0.3, 1 or 3 mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys. AZD-8529 (30 mg/kg) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats[1].


[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.

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