Structure-activity relationship of N-methyl-N-aralkylpeptidylamines as novel N-type calcium channel blockers

Article abstract of DOI:10.1016/S0960-894X(99)00359-5

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.