T R Ryder, L Y Hu, M F Rafferty, S M Lotarski, D M Rock, S J Stoehr, C P Taylor, M L Weber, G P Miljanich, E Millerman, B G Szoke
{"title":"Structure-activity relationship at the leucine side chain in a series of N,N-dialkyldipeptidyl-amines as N-type calcium channel blockers.","authors":"T R Ryder, L Y Hu, M F Rafferty, S M Lotarski, D M Rock, S J Stoehr, C P Taylor, M L Weber, G P Miljanich, E Millerman, B G Szoke","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>Exploration of the SAR around the leucine side chain in a series of N,N-dialkyldipeptidylamines with potent functional activity at N-type VSCC is presented. A novel analog is disclosed which possesses improved aqueous solubility, in vivo activity in an audiogenic seizure model, and reversible blockade in electrophysiological assays.</p>","PeriodicalId":11297,"journal":{"name":"Drug design and discovery","volume":"16 4","pages":"317-22"},"PeriodicalIF":0.0000,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug design and discovery","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
Abstract
Exploration of the SAR around the leucine side chain in a series of N,N-dialkyldipeptidylamines with potent functional activity at N-type VSCC is presented. A novel analog is disclosed which possesses improved aqueous solubility, in vivo activity in an audiogenic seizure model, and reversible blockade in electrophysiological assays.