1160184-89-3Relevant academic research and scientific papers
Discovery of DSP-1053, a novel benzylpiperidine derivative with potent serotonin transporter inhibitory activity and partial 5-HT1A receptor agonistic activity
Yoshinaga, Hidefumi,Nishida, Tomoaki,Sasaki, Izumi,Kato, Taro,Oki, Hitomi,Yabuuchi, Kazuki,Toyoda, Tomohiro
supporting information, p. 1614 - 1627 (2018/02/21)
We have previously shown that SMP-304, a serotonin uptake inhibitor with weak 5-HT1A partial agonistic activity, may act under high serotonin levels as a 5-HT1A antagonist that improves the onset of paroxetine in the rat swimming test. However, SMP-304 is mostly metabolized by CYP2D6, indicating limited efficacy among individuals and increased side effects. To reduce CYP2D6 metabolic contribution and enhance SERT/5-HT1A binding affinity, we carried out a series of substitutions at the bromine atom in the left part of the benzene ring of SMP-304 and replaced the right part of SMP-304 with a chroman-4-one. This optimization work led to the identification of the antidepressant candidate DSP-1053 as a potent SERT inhibitor with partial 5-HT1A receptor agonistic activity. DSP-1053 showed low CYP2D6 metabolic contribution and a robust increase in serotonin levels in the rat frontal cortex.
Extended fluorochromism of anthracene trimers with a meta-substituted triphenylamine or triphenylphosphine core
Li, Zhiou,Ishizuka, Hiromi,Sei, Yoshihisa,Akita, Munetaka,Yoshizawa, Michito
supporting information; experimental part, p. 1789 - 1794 (2012/09/07)
Combining meta-triphenylamine or triphenylphosphine with three anthracene fluorophores gives rise to fluorescent non-planar triskelions 1 and 2. The emissive properties of 1 are highly solvatochromic, yielding blue to pale green and even pale yellow fluor
A tubular macrocycle from covalently linked anthracenes and meta-phenylene spacers
Hagiwara, Keita,Sei, Yoshihisa,Akita, Munetaka,Yoshizawa, Michito
supporting information; experimental part, p. 7678 - 7680 (2012/09/21)
A novel tubular macrocycle containing four anthracene panels covalently linked by meta-phenylene spacers was synthesized. The tube is approximately 1 nm long with anthracene panels delimiting a columnar cavity with a diameter of ～1 nm and exhibits strong blue fluorescence.
BENZYLPIPERIZINE COMPOUND
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Page/Page column 12, (2010/05/13)
Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a met
Design and optimization of a substituted amino propanamide series of renin inhibitors for the treatment of hypertension
Chen, Austin,Bayly, Christopher,Bezen?on, Olivier,Richard-Bildstein, Sylvia,Dubé, Daniel,Dubé, Laurence,Gagné, Sébastien,Gallant, Michel,Gaudreault, Mireille,Grimm, Erich,Houle, Robert,Lacombe, Patrick,Laliberté, Sébastien,Lévesque, Jean-Fran?ois,Liu, Suzanna,MacDonald, Dwight,Mackay, Bruce,Martin, David,McKay, Dan,Powell, David,Remeň, L'ubo?,Soisson, Stephen,Toulmond, Sylvie
scheme or table, p. 2204 - 2209 (2010/06/19)
The discovery and SAR of a new series of substituted amino propanamide renin inhibitors are herein described. This work has led to the preparation of compounds with in vitro and in vivo profiles suitable for further development. Specifically, challenges p
RENIN INHIBITORS
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Page/Page column 20, (2009/07/17)
The present invention relates to piperidinyl-based renin inhibitor compounds having the formula containing amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.
