striatal neuron

Potent somatostatin receptor 1 (sst1) agonist; displays selectivity for sst1 (IC50 values are 30.9 nM, 345 nM, > 1 μM, > 10 μM and > 10μM for human sst1, sst3, sst4, sst2 and sst5 respectively). Attenuates somatostatin release in the rat nucleus accumbens

BRF110 is a brain penetrant, potent and selective agonist of nuclear receptor-related 1 (Nurr1):Retinoid X receptor α (RXRα) heterodimer. BRF110 is a neuroprotective agent that prevents dopaminergic neuron demise and striatal dopaminergic denervation in vivo against PD-causing toxins. It induced dopamine biosynthesis in vivo. BRF110 chronic dosing does not induce dyskinesia in mice model.

MTX115325 (Example 1) 是一种口服有效且脑渗透性的 USP30 抑制剂 (IC50=12 nM)，具备神经保护活性。MTX115325 增加线粒体外膜蛋白 TOM20（USP30底物）的泛素化 (EC50=32 nM)，并促进线粒体自噬。MTX115325 能防止多巴胺能神经元损失，保留纹状体多巴胺。