Abstract
1-Benzyl-N-(2,6-dimethylphenyl)piperidine-3-carboxamide and 4-benzyl-N-(2,6-dimethylphenyl)piperazine-2-carboxamide, two conformationally restricted analogues of tocainide, were designed and synthesized as voltage-gated skeletal muscle sodium channel blockers. They showed, with respect to tocainide, a marked increase in both potency and use-dependent block.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Molecular Structure
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Muscle, Skeletal / drug effects*
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Muscle, Skeletal / metabolism
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Myotonia*
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Sodium Channel Blockers / chemical synthesis*
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Sodium Channel Blockers / chemistry
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Sodium Channel Blockers / pharmacology*
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Structure-Activity Relationship
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Tocainide / analogs & derivatives
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Tocainide / chemical synthesis*
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Tocainide / chemistry
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Tocainide / pharmacology*
Substances
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Sodium Channel Blockers
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Tocainide