AZD-8529 mesylate 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 285 nM；在 20-25 M 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:ajcx29146
CAS:1314217-69-0
分子式:C25H28F3N5O6S
分子量：583.58
溶解度:DMSO: 41.67 mg/mL (71.40 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

AZD-8529 mesylate 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[1].

AZD-8529 mesylate potentiates the effects of glutamate at mGluR2 with an EC50 of 195 nM [1].AZD-8529 mesylate does not elicit antagonist responses on mGluRs at 25 μM[1].

AZD-8529 mesylate (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys[1]. AZD-8529 mesylate (30 mg/kg; i.p.) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats[1]. Animal Model: Sprague-Dawley 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.