Diaryldiamines with Dual Inhibition of the Histamine H3 Receptor and the Norepinephrine Transporter and the Efficacy of 4-(3-(Methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)napht

详细信息    查看全文

• 作者：Robert J. Altenbach ; Lawrence A. Black ; Marina I. Strakhova ; Arlene M. Manelli ; Tracy L. Carr ; Kennan C. Marsh ; Jill M. Wetter ; Erica J. Wensink ; Gin C. Hsieh ; Prisca Honore ; Tiffany Runyan Garrison
• 刊名：Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：November 11, 2010
• 年：2010
• 卷：53
• 期：21
• 页码：7869-7873
• 全文大小：770K
• 年卷期：v.53,no.21(November 11, 2010)
• ISSN：1520-4804

文摘

A series of compounds was designed as dual inhibitors of the H₃ receptor and the norepinephrine transporter. Compound 5 (rNET K_i = 14 nM; rH₃R K_i = 37 nM) was found to be efficacious in a rat model of osteoarthritic pain.