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。
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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