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

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• 作者：Yong-Jin Wu ; ^{yong-jin.wu@bms.com" class="auth_mail} ; Huan He ; Qi Gao ; Dedong Wu ; Robert Bertekap ; Ryan S. Westphal ; Snjezana Lelas ; Amy Newton ; Tanya Wallace ; Matthew Taber ; Carl Davis ; John E. Macor ; Joanne Bronson
• 关键词：NK1 receptor (NK1R) antagonist ; Serotonin reuptake transporter (SERT) inhibitor ; Dual NK1 receptor antagonists&ndash ; serotonin reuptake transporter inhibitor
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：15 March, 2014
• 年：2014
• 卷：24
• 期：6
• 页码：1611-1614
• 全文大小：1316 K

文摘

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.