AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC 50 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.
性状
Oil
IC50 & Target[1][2]
mGluR2 285 nM (EC50)
体外研究(In Vitro)
AZD-8529 potentiates the effects of glutamate at mGluR2 with an EC50 of 195 nM.AZD-8529 does not elicit antagonist responses on mGluRs at 25 μM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
AZD-8529 (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys.
AZD-8529 (30 mg/kg; i.p.) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 62.5 mg/mL (128.21 mM; Need ultrasonic)配制储备液