Abstract
A series of new 6-styryl-naphthalene-2-amidrazone derivatives were synthesized and evaluated as potential ASIC1a inhibitors. Among them, compound 5e showed the most activity to inhibit [Ca2+]i. elevation in acid-induced articular chondrocytes. Together with the important role of ASIC1a in the pathogenesis of tissue acidification diseases including rheumatoid arthritis, these results might provide a meaningful hint or inspiration in developing drugs targeting at tissue acidification diseases.
Keywords:
ASIC activity; Amidrazone; Articular chondrocytes; [Ca(2+)](i).
Copyright © 2018 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acid Sensing Ion Channels / chemistry
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Acid Sensing Ion Channels / metabolism
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Animals
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Calcium / 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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Cell Survival / drug effects
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Cells, Cultured
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Chondrocytes / cytology
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Chondrocytes / metabolism
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Drug Design*
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Naphthalenes / chemistry
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Rats
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Sodium Channel Agonists / chemical synthesis*
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Sodium Channel Agonists / chemistry
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Sodium Channel Agonists / pharmacology
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Structure-Activity Relationship
Substances
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Acid Sensing Ion Channels
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Carboxylic Acids
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Naphthalenes
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Sodium Channel Agonists
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naphthalene
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Calcium