化学
神经保护
兴奋剂
药理学
受体
斑马鱼
对接(动物)
毛茛
结构-活动关系
部分
功能选择性
失忆症
化学合成
小分子
体外
配体(生物化学)
神经退行性变
药物发现
神经毒素
码头
Sigma-1受体
神经科学
选择性
离解(化学)
疾病
立体化学
离解率
分子模型
体内
变构调节
生物活性
药品
计算生物学
作者
Francesco Mastropasqua,Anna Teresa Lisi,Lucie Crouzier,Gabriella Rosanna Musillo,Francesca Serena Abatematteo,Mauro Niso,Benjamin Delprat,Nicola Antonio Colabufo,Vittoria Nanna,Giuseppe Felice Mangiatordi,Pietro Delre,Tina Spalholz,Matilde Colella,Winnie Deuther‐Conrad,Fulvio Loiodice,Tangui Maurice,Antonio Laghezza,Carmen Abate
标识
DOI:10.1021/acs.jmedchem.5c03240
摘要
to assess hyperlocomotion reduction. Seven hit compounds were selected for the BiP-S1R dissociation as a measure of their agonist activity, followed by the preclinical evaluation of their activity against Alzheimer's Disease (AD) in mice. These phenoxyethylpiperidines demonstrated to potently prevent AD-like amnesia without toxicity, appearing as promising agents for further preclinical studies against neurodegeneration.
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