A potent and selective indole N-type calcium channel (Cab>vb>2.2) blocker for the treatment of pain

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• 作者：Sriram Tyagarajan^a ; ^{sriram_tyagarajan@merck.com} ; Prasun K. Chakravarty^a ; Min Park^a ; Bishan Zhou^a ; James B. Herrington^b ; Kevin Ratliff^b ; Randall M. Bugianesi^b ; Brande Williams^b ; Rodolfo J. Haedo^b ; Andrew M. Swensen^b ; Vivien A. Warren^b ; McHardy Smith^b ; Maria Garcia^b ; Gregory J. Kaczorowski^b ; Owen B. McManus^b ; Kathryn A. Lyons^c ; Xiaohua Li^c ; Maria Madeira^c ; Bindhu Karanam^c ; Mitchell Green^c ; Michael J. Forrest^d ; Catherine Abbadie^d ; Erin McGowan^d ; Shruti Mistry^d ; Nina Jochnowitz^d ; Joseph L. Duffy^a
• 关键词：Pain ; N-type calcium channel ; Cab>vb>2.2 blockers ; Indoles ; Chung model
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2011
• 出版时间：15 January 2011
• 年：2011
• 卷：21
• 期：2
• 页码：869-873
• 全文大小：1247 K

文摘

N-type calcium channels (Cab>vb>2.2) have been shown to play a critical role in pain. A series of low molecular weight 2-aryl indoles were identified as potent Cab>vb>2.2 blockers with good in vitro and in vivo potency.