VU0238429

一种毒蕈碱型M5受体的正向别构调节剂（在钙离子动员实验中EC₅₀=1.16µM）；在表达人受体的CHO细胞中，对M5 mAChRs的选择性高于M1、M2、M3和M4 mAChRs（在钙离子动员实验中，对所有这些受体的EC₅₀均>30µM）；在小鼠中，以10mg/kg剂量减少DOI诱导的头扭行为；单独给药或与GS-39783联合使用时，能够逆转MK-801诱导的小鼠新物体识别测试中的记忆缺陷。A muscarinic M5 receptor positive allosteric modulator (EC50 = 1.16 µM in a calcium mobilization assay); selective for M5 mAChRs over M1, M2, M3, and M4 mAChRs in CHO cells expressing the human receptors (EC50s = >30 µM for all in calcium mobilization assays); reduces DOI-induced head-twitch behavior in mice at 10 mg/kg; reverses MK-801-induced memory deficits in the novel object recognition test in mice when administered alone or in combination with GS-39783.分子式C17H12F3NO4分子量351.3O=C1C(N(CC2=CC=C(C=C2)OC)C3=CC=C(C=C13)OC(F)(F)F)=O