217172-32-2Relevant academic research and scientific papers
N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers
Hu, Lain-Yen,Ryder, Todd R.,Rafferty, Michael F.,Cody, Wayne L.,Lotarski, Susan M.,Miljanich, George P.,Millerman, Elizabeth,Rock, David M.,Song, Yuntao,Stoehr, Sally J.,Taylor, Charles P.,Weber, Mark L.,Szoke, Balazs G.,Vartanian, Mark G.
, p. 907 - 912 (1999)
Selective N-type voltage sensitive calcium channel (VSCC) blockers have shown utility in several models of stroke and pain. We are especially interested in small molecule N-type calcium channel blockers for therapeutic use. Herein, we report a series of N,N-dialkyl-dipeptidylamines with potent functional activity at N-type VSCCs and in vivo efficacy. The synthesis, SAR, and pharmacological evaluation of this series are discussed.
Structure-activity relationship of N-methyl-N-aralkylpeptidylamines as novel N-type calcium channel blockers
Hu, Lain-Yen,Ryder, Todd R.,Rafferty, Michael F.,Dooley, David J.,Geer, Joann J.,Lotarski, Susan M.,Miljanich, George P.,Millerman, Elizabeth,Rock, David M.,Stoehr, Sally J.,Szoke, Balazs G.,Taylor, Charles P.,Vartanian, Mark G.
, p. 2151 - 2156 (2007/10/03)
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 IMR32 assays). SAR and pharmacological evaluation of this series are described.
