Benzamide derivatives as blockers of Kv1. 3 ion channel

…, JL Goulet, XJ Hong, GJ Kaczorowski, F Kayser…

Index: Miao, Shouwu; Bao, Jianming; Garcia, Maria L.; Goulet, Joung L.; Hong, Xingfang J.; Kaczorowski, Gregory J.; Kayser, Frank; Koo, Gloria C.; Kotliar, Andrew; Schmalhofer, William A.; Shah, Kashmira; Sinclair, Peter J.; Slaughter, Robert S.; Springer, Marty S.; Staruch, Mary Jo; Tsou, Nancy N.; Wong, Frederick; Parsons, William H.; Rupprecht, Kathleen M. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 6 p. 1161 - 1164

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Citation Number: 23

Abstract

The voltage-gated potassium channel, Kv1. 3, is present in human T-lymphocytes. Blockade of Kv1. 3 results in T-cell depolarization, inhibition of T-cell activation, and attenuation of immune responses in vivo. A class of benzamide Kv1. 3 channel inhibitors has been identified. The structure–activity relationship within this class of compounds in two functional assays, Rb_Kv and T-cell proliferation, is presented. In in vitro assays, trans isomers ...