{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Tarcha EJ"],"funding":["NIAID NIH HHS","NINDS NIH HHS"],"pagination":["642-53"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC3422530"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["342(3)"],"pubmed_abstract":["The Kv1.3 channel is a recognized target for pharmaceutical development to treat autoimmune diseases and organ rejection. ShK-186, a specific peptide inhibitor of Kv1.3, has shown promise in animal models of multiple sclerosis and rheumatoid arthritis. Here, we describe the pharmacokinetic-pharmacodynamic relationship for ShK-186 in rats and monkeys. The pharmacokinetic profile of ShK-186 was evaluated with a validated high-performance liquid chromatography-tandem mass spectrometry method to measure the peptide's concentration in plasma. These results were compared with single-photon emission computed tomography/computed tomography data collected with an ¹¹¹In-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-conjugate of ShK-186 to assess whole-blood pharmacokinetic parameters as w"],"journal":["The Journal of pharmacology and experimental therapeutics"],"pubmed_title":["Durable pharmacological responses from the peptide ShK-186, a specific Kv1.3 channel inhibitor that suppresses T cell mediators of autoimmune disease."],"pmcid":["PMC3422530"],"funding_grant_id":["R01 NS048252","R43-AI085691","R43 AI085691","R01-NS48252"],"pubmed_authors":["Bailey D","Slauter R","Norton K","Munoz-Elias EJ","Tjong I","Hu X","Beeton C","Hansen Z","Tarcha EJ","Boley SE","Sams J","Nguyen H","Ruppert GW","Knapp B","Upadhyay SK","Pennington MW","Kentala D","Chandy KG","Banks A","Chi V","Iadonato SP","Londono LM"],"additional_accession":[]},"is_claimable":false,"name":"Durable pharmacological responses from the peptide ShK-186, a specific Kv1.3 channel inhibitor that suppresses T cell mediators of autoimmune disease.","description":"The Kv1.3 channel is a recognized target for pharmaceutical development to treat autoimmune diseases and organ rejection. ShK-186, a specific peptide inhibitor of Kv1.3, has shown promise in animal models of multiple sclerosis and rheumatoid arthritis. Here, we describe the pharmacokinetic-pharmacodynamic relationship for ShK-186 in rats and monkeys. The pharmacokinetic profile of ShK-186 was evaluated with a validated high-performance liquid chromatography-tandem mass spectrometry method to measure the peptide's concentration in plasma. These results were compared with single-photon emission computed tomography/computed tomography data collected with an ¹¹¹In-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-conjugate of ShK-186 to assess whole-blood pharmacokinetic parameters as w","dates":{"release":"2012-01-01T00:00:00Z","publication":"2012 Sep","modification":"2026-05-04T00:57:08.385Z","creation":"2019-03-27T00:57:00Z"},"accession":"S-EPMC3422530","cross_references":{"pubmed":["22637724"],"doi":["10.1124/jpet.112.191890"]}}