Benzamide derivatives as blockers of Kv1.3 ion channel |
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| Authors: | 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 |
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| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. bao_jianming@merck.com |
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| 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 display moderate selectivity for binding to Kv1.3 over other Kv1.x channels present in human brain. |
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