Structure-activity relationship of N-methyl-N-aralkyl-peptidylamines as novel N-type calcium channel blockers.
Basic Information
ID: ALA1131814
Journal: Bioorg Med Chem Lett
Title: Structure-activity relationship of N-methyl-N-aralkyl-peptidylamines as novel N-type calcium channel blockers.
Authors: Hu LY, Ryder TR, Rafferty MF, Dooley DJ, Geer JJ, Lotarski SM, Miljanich GP, Millerman E, Rock DM, Stoehr SJ, Szoke BG, Taylor CP, Vartanian MG.
Abstract: Selective N-type voltage sensitive calcium channel (VSCC) blockers have shown efficacy in several animal models of stroke and pain. In the process of searching for small molecule N-type calcium channel blockers, we have identified a series of N-methyl-N-aralkyl-peptidylamines with potent functional activity at N-type VSCCs. The most active compound discovered in this series is PD 173212 (11, IC50 = 36 nM in the IMR-32 assays). SAR and pharmacological evaluation of this series are described.
CiteXplore: 10465535
DOI: 10.1016/s0960-894x(99)00359-5
Patent ID: ┄