Channelpedia

PubMed 12643934


Referenced in Channelpedia wiki pages of: none

Automatically associated channels: Kv1.3



Title: Benzamide derivatives as blockers of Kv1.3 ion channel.

Authors: Shouwu Miao, Jianming Bao, Maria L Garcia, Joung L Goulet, Xingfang J Hong, Gregory J Kaczorowski, Frank Kayser, Gloria C Koo, Andrew Kotliar, William A Schmalhofer, Kashmira Shah, Peter J Sinclair, Robert S Slaughter, Marty S Springer, Mary Jo Staruch, Nancy N Tsou, Frederick Wong, William H Parsons, Kathleen M Rupprecht

Journal, date & volume: Bioorg. Med. Chem. Lett., 2003 Mar 24 , 13, 1161-4

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/12643934


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.