Abstract
A series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide derivatives were synthesized and evaluated for their activity as allosteric modulators of kainate-activated currents in primary cultures of cerebellar granule neurons. Substitution of different groups at the 3-position of the benzothiadiazine ring distinguished between positive and negative allosteric modulatory properties.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Allosteric Regulation
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Animals
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Benzothiadiazines / chemical synthesis*
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Benzothiadiazines / chemistry
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Benzothiadiazines / pharmacology
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Cell Line
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Cerebellum / cytology
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Excitatory Amino Acid Agonists / pharmacology
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Kainic Acid / pharmacology
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Patch-Clamp Techniques
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Rats
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Receptors, AMPA / drug effects*
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Receptors, AMPA / physiology
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Receptors, Kainic Acid / drug effects*
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Receptors, Kainic Acid / physiology
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Stereoisomerism
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Structure-Activity Relationship
Substances
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3,4-dihydro-1,2,4-benzothiadiazine-1,1-dioxide
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Benzothiadiazines
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Excitatory Amino Acid Agonists
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Receptors, AMPA
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Receptors, Kainic Acid
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Kainic Acid