Discovery of diphenyl amine based sodium channel blockers, effective against hNa v 1.2

DP Hudgens, C Taylor, TW Batts, MK Patel…

文献索引：Hudgens, Debjani P.; Taylor, Catherine; Batts, Timothy W.; Patel, Manoj K.; Brown, Milton L. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 24 p. 8366 - 8378

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被引用次数: 12

摘要

The development of new therapies for chronic pain is an area of unmet medical need. Central to pathways of chronic pain is the upregulation of voltage-gated sodium channels. The use of tricyclic antidepressants, which also have sodium channel activity, in chronic pain therapy prompted us to develop novel compounds from this scaffold. Herein, we show that the tricyclic moiety is not needed for effective inhibition of the [3H]-BTX binding site and ...