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Discovery of a cyclopentylamine as an orally active dual NK1 receptor antagonist–serotonin reuptake transporter inhibitor.

Authors :
Wu, Yong-Jin
He, Huan
Gao, Qi
Wu, Dedong
Bertekap, Robert
Westphal, Ryan S.
Lelas, Snjezana
Newton, Amy
Wallace, Tanya
Taber, Matthew
Davis, Carl
Macor, John E.
Bronson, Joanne
Source :
Bioorganic & Medicinal Chemistry Letters. Mar2014, Vol. 24 Issue 6, p1611-1614. 4p.
Publication Year :
2014

Abstract

Abstract: Cyclopentylamine 4 was identified as a potent dual NK1R antagonist–SERT inhibitor. This compound demonstrated significant oral activity in the gerbil forced swimming test, suggesting that dual NK1R antagonists–SERT inhibitors may be useful in treating depression disorders. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
24
Issue :
6
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
94788343
Full Text :
https://doi.org/10.1016/j.bmcl.2014.01.036