874375-73-2Relevant academic research and scientific papers
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression
Wu, Yong-Jin,He, Huan,Bertekap, Robert,Westphal, Ryan,Lelas, Snjezana,Newton, Amy,Wallace, Tanya,Taber, Matthew,Davis, Carl,MacOr, John E.,Bronson, Joanne
, p. 2217 - 2228 (2013/05/08)
This report describes the synthesis, structure-activity relationships and activity of piperidine, homopiperidine, and azocane derivatives combining NK1 receptor (NK1R) antagonism and serotonin reuptake transporter (SERT) inhibition. Our studies culminated in the discovery of piperidine 2 and homopiperidine 8 as potent dual NK1R antagonists-SERT inhibitors. Compound 2 demonstrated significant activity in the gerbil forced swimming test, suggesting that dual NK1R antagonists-SERT inhibitors may be useful in treating depression disorders.
Cyclopentylamine and cyclohexylamine derivatives as NK-1/SSRI antagonists
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Page/Page column 8; 9, (2010/02/15)
The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment of the disclosure relates to compounds of Formula (I); or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compounds are useful for the useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.
