| Description | Dipraglurant (ADX48621) is a negative alteration modulator (NAM) of mGluR5 that inhibits dyskinesia in the LID macaque model. |
| In vitro | 作用于 mGlu 受体的新型负变构调节剂（NAM）双歧剂 Dipraglurant （1-10μM;15分钟）抵消了 D2R 激动剂喹吡罗或（NPEC-多巴胺）在两种模型中诱导的异常膜反应和钙升高[2]。 |
| In vivo | Dipraglurant（3-30 mg/kg;单次口服）具有良好的药代动力学，可减少左旋多巴诱导的舞蹈症和肌张力障碍，但并且不会干扰左旋多巴治疗帕金森病残疾猕猴的疗效[1]。 |
| Target activity | mGluR5:21 nM |
| Synonyms | ADX48621 |
| molecular weight | 265.29 |
| Molecular formula | C16H12FN3 |
| CAS | 872363-17-2 |
| Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 40 mg/mL (150.78 mM) |
| References | 1. Bezard E, et al. The mGluR5 negative allosteric modulator dipraglurant reduces dyskinesia in the MPTP macaque model. Mov Disord. 2014 Jul;29(8):1074-9. 2. Sciamanna G, et al. Negative allosteric modulation of mGlu5 receptor rescues striatal D2 dopamine receptor dysfunction in rodent models of DYT1 dystonia. Neuropharmacology. 2014 Oct;85:440-50. |