| Description | 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. |
| In vitro | AZD-8529在mGluR2上增强谷氨酸的效应（EC50: 195 nM）。在25 μM浓度下，AZD-8529 不引发mGluRs的拮抗反应。 |
| In vivo | AZD-8529（30 mg/kg；i.p.）能够降低自由活动大鼠伏隔核壳区域因尼古丁引起的多巴胺外泌增加。同时，AZD-8529（0.3 mg/kg；i.m.）减少了松鼠猴因尼古丁原发性诱导和线索诱导的复吸行为。 |
| Target activity | mGluR2:（EC50）285 nM |
| molecular weight | 583.58 |
| Molecular formula | C25H28F3N5O6S |
| CAS | 1314217-69-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 41.67 mg/mL (71.40 mM), Sonication is recommended. |
| References | 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. |