HT-2157

一种GAL3受体拮抗剂（Ki=17nM），对GAL3的选择性高于GAL1和GAL2（对后两者的Ki值均>10µM）。该拮抗剂在10µM浓度下可诱导多种细胞类型的凋亡，包括HL-60白血病细胞、BV-2小鼠小胶质细胞以及分离的人类外周血单个核细胞（PBMCs）。此外，在动物实验中，该拮抗剂以30mg/kg剂量显著减少大鼠对酒精、蔗糖和阿斯巴甜的自我摄取行为；在Vogel惩罚性饮水实验中增加饮水行为，并在强迫游泳实验中减少大鼠的不动时间，分别显示出抗焦虑和抗抑郁样活性。A GAL3 receptor antagonist (Ki = 17 nM); selective for GAL3 over GAL1 and GAL2 (Kis = >10 µM for both); induces apoptosis in various cell types, including HL-60 leukemia and BV-2 murine microglial cells, as well as isolated human PBMCs at 10 µM; decreases operant alcohol, sucrose, and saccharin self-administration in rats at 30 mg/kg; increases drinking in the Vogel punished drinking task and reduces immobility time in the forced swim test in rats, indicating anxiolytic- and antidepressant-like activities, respectively, at 3 and 10 mg/kg.分子式C21H13F3N2O分子量366.3O=C1C(C2=C(N1C3=CC=CC=C3)C=CC=C2)=NC4=CC(C(F)(F)F)=CC=C4