Abstract
Acylated and aroylated hydrazinoclozapines are highly potent dopamine D(1) antagonists that show remarkable selectivity over other dopamine receptors. The most potent compound in this series is the 2,6-dimethoxybenzhydrazide 33 with a D(1)K(i) of 1.6 nM and 212-fold selectivity over D(2) receptor.
MeSH terms
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Clozapine / chemical synthesis
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Clozapine / chemistry*
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Clozapine / classification
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Clozapine / pharmacology*
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Dopamine Antagonists / chemical synthesis*
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Dopamine Antagonists / chemistry
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Dopamine Antagonists / classification
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Dopamine Antagonists / pharmacology*
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Dopamine D2 Receptor Antagonists
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Hydrazines / chemistry*
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Molecular Structure
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Receptors, Dopamine D1 / antagonists & inhibitors*
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Receptors, Dopamine D1 / metabolism
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Receptors, Dopamine D2 / metabolism
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Structure-Activity Relationship
Substances
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Dopamine Antagonists
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Dopamine D2 Receptor Antagonists
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Hydrazines
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Receptors, Dopamine D1
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Receptors, Dopamine D2
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hydrazine
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Clozapine