Author/Authors :
Lain-Yen Hu، نويسنده , , Todd Ryder R.، نويسنده , , Michael F. Rafferty، نويسنده , , David J. Dooley، نويسنده , , Joann J. Geer، نويسنده , , Susan M. Lotarski، نويسنده , , George P. Miljanich، نويسنده , , Elizabeth Millerman، نويسنده , , David M. Rock، نويسنده , , Sally J. Stoehr، نويسنده , , Balazs G. Szoke، نويسنده , , Charles P. Taylor، نويسنده , , Mark G. Vartanian، نويسنده ,
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.
