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。
货号:ajcx12486
CAS:1092453-15-0
分子式:C24H24F3N5O3
分子量：487.47
溶解度:DMSO: 62.5 mg/mL (128.21 mM)
纯度：98%
存储：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.