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生化/生理作用
Siramesine is a blood-brain barrier penetrant, selective and potent sigma-2 receptor agonist, which exhibits potent and very long-lasting anxiolytic effects in rodents. Also, siramesine is a lysosome-destabilizing agent that causes lysosomal cell death in varies immortalized and cancer cell lines.
Siramesine is a blood-brain barrier penetrant, selective and potent sigma-2 receptor agonist.
Siramesine or Lu 28-179 (1′-[4-[1-(4-fluorophenyl)-1H-indol-3-yl]-1-butyl]-spiro[isobenzofuran-1(3H),4′-piperidine]) is considered as a drug for depression and anxiety. This lysosomotropic agent stimulates mitochondrial membrane potential (MMP) reduction and the production of ROS (reactive oxygen species).
特点和优势
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储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Z H Zhang et al.
Zhonghua xue ye xue za zhi = Zhonghua xueyexue zazhi, 42(5), 407-414 (2021-07-05)
Objective: To clarify the effects of bortezomib combined with or without siramesine on the proliferation of multiple myeloma cell lines, the expression changes of transcription factor EBC (TFEB) nuclear translocation and the level of autophagy, and to provide basis for
Monitoring recovery after CNS demyelination, a novel tool to de-risk pro-remyelinating strategies.
Henriet, et al.
Brain, 146, 2453-2463 (2023)
Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes.
Cesen MH, et al.
Cell Death & Disease, 4(10), e818-e818 (2013)
Damir Bojadzic et al.
Frontiers in pharmacology, 11, 600372-600372 (2021-02-02)
Due to our interest in the chemical space of organic dyes to identify potential small-molecule inhibitors (SMIs) for protein-protein interactions (PPIs), we initiated a screen of such compounds to assess their inhibitory activity against the interaction between SARS-CoV-2 spike protein
Ferroptosis is induced following siramesine and lapatinib treatment of breast cancer cells.
Ma S, et al.
Cell Death & Disease, 7(7), e2307-e2307 (2016)
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