| Description | AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux. |
| In vitro | AZD9272 (10 μM) 在背景的GHEK细胞中对10 μM ATP的反应未表现出减少。AZD9272浓度的增加导致DHPG的效能和最大反应减弱。[1] AZD9272以浓度依赖的方式完全逆转了人类mGluR5-GHEK细胞中由谷氨酸（EC80=80 μM）刺激的磷脂酰肌醇水解，其IC50为26±3 nM（n=21）。[1] |
| In vivo | AZD 9272 (3 μmol/kg; 单次静脉注射) 从血浆中的清除具有终末半衰期介于2至6小时之间。口服给药后的终末半衰期与静脉给药后的半衰期相似。稳态时的分布体积对于AZD9272而言是中等的。[1] AZD9272 (2.84 mg/kg) 在给药后20小时内引起超过80%，通常超过99%的MTEP适应性反应，到给药后24小时时，反应下降至大约20%，产生21.93小时的t1/2，并且对反应率没有系统性影响。AZD9272造成超过90%的MTEP适应性反应的首个时间点是在给药后30分钟。[2] |
| Target activity | mGluR5 (human):7.6±1.1 nM, mGluR5 (rat):2.6±0.3 nM |
| molecular weight | 284.22 |
| Molecular formula | C14H6F2N4O |
| CAS | 327056-26-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: ＜1 mg/mL (insoluble or slightly soluble) |
| References | 1. Swedberg MD, et al. AZD9272 and AZD2066: selective and highly central nervous system penetrant mGluR5 antagonists characterized by their discriminative effects. J Pharmacol Exp Ther. 2014 Aug;350(2):212-22. 2. Raboisson P, et al. Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6974-9. |