69160-56-1Relevant academic research and scientific papers
Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors
Zhang, Mingzhu,Jovic, Florence,Vickers, Troy,Dyck, Brian,Tamiya, Junko,Grey, Jonathan,Tran, Joe A.,Fleck, Beth A.,Pick, Rebecca,Foster, Alan C.,Chen, Chen
scheme or table, p. 3682 - 3686 (2009/04/06)
Compounds with various activities and selectivities were discovered through structure-activity relationship studies of bicifadine analogs as monoamine transporter inhibitors. The norepinephrine-selective 2-thienyl compound S-6j was efficacious in a rodent
1-Aryl-2-(aminomethyl)cyclopropanecarboxylic Acid Derivatives. A New Series of Potential Antidepressants
Bonnaud, Bernard,Cousse, Henri,Mouzin, Gilbert,Briley, Mike,Stenger, Antoine,et al.
, p. 318 - 325 (2007/10/02)
A series of 1-aryl-2-(aminomethyl)cyclopropanecarboxylic acid derivatives were synthesized and evaluated as potential antidepressants.Compounds with the Z configuration were synthesized from 1-aryl-2-oxo-3-oxabicyclohexane and those with E configuration from (E)-1-phenyl-2-(hydroxymethyl)cyclopropanecarboxylic acid.The compounds were evaluated in animal tests designed to reveal potential antidepressant activity and the existence of undesirable side effects.Several derivatives were more active than imipramine and desipramine.On the basis of its activity in pharmacological animal tests of antidepressant activity and its potential lack of side effects, 1-phenyl-1--2-(aminomethyl)cyclopropane hydrochloride, midalcipran (INN), was selected for further development.This compound is currently in phase III clinical evaluation.
