826-01-7Relevant articles and documents
Ulotaront: A TAAR1 Agonist for the Treatment of Schizophrenia
Heffernan, Michele L. R.,Herman, Lee W.,Brown, Scott,Jones, Philip G.,Shao, Liming,Hewitt, Michael C.,Campbell, John E.,Dedic, Nina,Hopkins, Seth C.,Koblan, Kenneth S.,Xie, Linghong
, p. 92 - 98 (2021/12/17)
Ulotaront (SEP-363856) is a trace-amine associated receptor 1 (TAAR1) agonist with 5-HT1A receptor agonist activity in Phase 3 clinical development, with FDA Breakthrough Therapy Designation, for the treatment of schizophrenia. TAAR1 is a G-protein-coupled receptor (GPCR) that is expressed in cortical, limbic, and midbrain monoaminergic regions. It is activated by endogenous trace amines, and is believed to play an important role in modulating dopaminergic, serotonergic, and glutamatergic circuitry. TAAR1 agonism data are reported herein for ulotaront and its analogues in comparison to endogenous TAAR1 agonists. In addition, a human TAAR1 homology model was built around ulotaront to identify key interactions and attempt to better understand the scaffold-specific TAAR1 agonism structure-activity relationships.
Highly enantioselective henry reactions in water catalyzed by a copper tertiary amine complex and applied in the synthesis of (S)-N-trans-feruloyl octopamine
Lai, Guoyin,Guo, Fengfeng,Zheng, Yueqin,Fang, Yang,Song, Haigang,Xu, Kun,Wang, Sujing,Zha, Zhenggen,Wang, Zhiyong
supporting information; experimental part, p. 1114 - 1117 (2011/03/21)
It's in the water! A new copper tertiary amine complex was prepared and applied in asymmetric Henry reactions in water and in the short synthesis of (S)-N-trans-feruloyl octopamine. This catalytic system provided an approach to the enantioselective Henry reaction of aldehydes with hydroxyl substituents (see graphic).
COMPOUNDS AND METHODS FOR TREATMENT OF CANCER AND MODULATION OF PROGRAMMED CELL DEATH FOR MELANOMA AND OTHER CANCER CELLS
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Page/Page column 39, (2008/06/13)
Compounds and related methods for synthesis, and the use of compounds and combination therapies for the treatment of cancer and modulation of apoptosis in cells are disclosed. The generation of synthetic combinatorial libraries and the evaluation of library member compounds regarding induction of apoptosis selectively in cancer cells are disclosed. Compounds, methods of making the compounds, and therapeutic methods with application against breast cancer cells, melanoma cancer cells, colon cancer cells, and other cancer cells are described.