AZD-8529 mesylate 是高度选择性的可口服mGluR2正向调节剂,EC50值为 285 nM。它在 20-25 M 时,对 mGluR1、3、4、5、6、7 和 8 亚型没有显示正变构调节剂反应。
产品描述
AZD-8529 mesylate is a highly selective, and orally bioavailable positive allosteric modulator of mGluR2 (EC50: 285 nM). It shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
体外活性
AZD-8529 potentiates the effects of glutamate at mGluR2 (EC50: 195 nM). It does not elicit antagonist responses on mGluRs at 25 μM.
体内活性
AZD-8529 (30 mg/kg; i.p.) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats. AZD-8529 (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys.
Cas No.
1314217-69-0
分子式
C25H28F3N5O6S
分子量
583.58
储存和溶解度
DMSO:41.67 mg/mL (71.40 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years