LM-10

TDO抑制剂(IC50=2µM)；10µM时对TDO的选择性优于IDO、MAO-A和MAO-B，以及一组各种受体和转运蛋白；使用用P815抗原P1A免疫的小鼠，逆转TDO过表达P815B肥大细胞瘤同源模型中的肿瘤免疫抗性；在50mg/kg剂量下，防止黑质中多巴胺能神经元数量减少、小胶质细胞体积增加，并抑制鱼藤酮诱发的帕金森病小鼠模型中肠道运输减少。A TDO inhibitor (IC50 = 2 µM); selective for TDO over IDO, MAO-A, and MAO-B, as well as a panel of various receptors and transporters, at 10 µM; reverses tumoral immune resistance in a TDO-overexpressing P815B mastocytoma syngeneic model using mice immunized with the P815 antigen P1A; prevents decreases in the number of dopaminergic neurons and increases in microglial cell volume in the substantia nigra and inhibits decreases in intestinal transit in a mouse model of rotenone-induced Parkinson's disease at 50 mg/kg.分子式C11H8FN5分子量229.2FC1=CC=C2C(/C=C/C3=NN=NN3)=CNC2=C1