Benzamide derivatives as blockers of Kv1.3 ion channel

Autor:	Maria L. Garcia, Frank Kayser, Peter J. Sinclair, Mary Jo Staruch, Andrew Kotliar, Nancy N. Tsou, William H. Parsons, Marty S. Springer, Gloria C. Koo, Kathleen M. Rupprecht, William A. Schmalhofer, Gregory J. Kaczorowski, Robert S. Slaughter, Joung L. Goulet, Kashmira Shah, Jianming Bao, Xingfang J. Hong, Frederick Wong, Shouwu Miao
Rok vydání:	2003
Předmět:	Potassium Channels medicine.drug_class Stereochemistry T-Lymphocytes Clinical Biochemistry Pharmaceutical Science Carboxamide In Vitro Techniques complex mixtures Biochemistry Structure-Activity Relationship chemistry.chemical_compound In vivo Drug Discovery Potassium Channel Blockers medicine Humans natural sciences Benzamide Molecular Biology Ion channel Brain Chemistry Kv1.3 Potassium Channel urogenital system Chemistry Organic Chemistry Stereoisomerism Depolarization Potassium channel In vitro nervous system Potassium Channels Voltage-Gated Benzamides Molecular Medicine biological phenomena cell phenomena and immunity Selectivity Rubidium Radioisotopes Cell Division
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 13:1161-1164
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd33db6982167b726fc36794cabfa008 https://doi.org/10.1016/s0960-894x(03)00014-3 Zobrazit plný text záznamu Full Text from ScienceDirect