Abstract
A structure-activity relationship study of 6-unsubstituted-1,4-dihydropyridine and 2,6-unsubstituted-1,4-dihydropyridine derivatives was conducted in an attempt to discover N-type calcium channel blockers that were highly selective over L-type calcium channel blockers. Among the tested compounds, (+)-4-(3,5-dichloro-4-methoxy-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid 3-cinnamyl ester was found to be an effective and selective N-type calcium channel blocker with oral analgesic potential.
Copyright © 2012 Elsevier Ltd. All rights reserved.
MeSH terms
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Administration, Oral
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Analgesics / chemical synthesis
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Analgesics / chemistry*
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Analgesics / pharmacology
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Animals
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Calcium Channel Blockers / chemical synthesis
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Calcium Channel Blockers / chemistry*
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Calcium Channel Blockers / pharmacology
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Calcium Channels, N-Type / chemistry*
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Calcium Channels, N-Type / metabolism
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Carboxylic Acids / chemical synthesis
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Carboxylic Acids / chemistry*
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Carboxylic Acids / pharmacology
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Dihydropyridines / chemistry*
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Drug Evaluation, Preclinical
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Formaldehyde / toxicity
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Pain Measurement / drug effects
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Rats
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Structure-Activity Relationship
Substances
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Analgesics
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Calcium Channel Blockers
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Calcium Channels, N-Type
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Carboxylic Acids
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Dihydropyridines
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Formaldehyde
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1,4-dihydropyridine