| Literature DB >> 10465535 |
L Y Hu1, T R Ryder, M F Rafferty, D J Dooley, J J Geer, S M Lotarski, G P Miljanich, E Millerman, D M Rock, S J Stoehr, B G Szoke, C P Taylor, M G Vartanian.
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.Entities:
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Year: 1999 PMID： 10465535 DOI： 10.1016/s0960-894x(99)00359-5
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823