Bioorganic and Medicinal Chemistry Letters p. 2151 - 2156 (1999)
Update date:2022-08-05
Topics:
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.
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.
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