1429045-52-2Relevant articles and documents
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.