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生物化学的／生理学的作用
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 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).
特徴および利点
This compound is a featured product for Neuroscience research. Click here to discover more featured Neuroscience products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
試験成績書（COA）
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Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes.
Cesen MH, et al.
Cell Death & Disease, 4(10), e818-e818 (2013)
Monitoring recovery after CNS demyelination, a novel tool to de-risk pro-remyelinating strategies.
Henriet, et al.
Brain, 146, 2453-2463 (2023)
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
Ferroptosis is induced following siramesine and lapatinib treatment of breast cancer cells.
Ma S, et al.
Cell Death & Disease, 7(7), e2307-e2307 (2016)
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
資料
DISCOVER Bioactive Small Molecules for Neuroscience
関連コンテンツ
神経科学分野における低分子生理活性物質の創薬研究
ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
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