Abstract
A series of novel 1,3-benzodiazapine based D1 antagonists was designed according to the understanding of pharmacophore models derived from SCH 23390 (1b), a potent and selective D1 antagonist. The new design features an achiral cyclic-amidine that maintains desired basicity. Solid phase synthesis was developed for SAR development of the novel dopamine antagonists.
MeSH terms
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Benzazepines / chemistry
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Benzazepines / pharmacology
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Benzodiazepines / chemical synthesis
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Benzodiazepines / chemistry*
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Benzodiazepines / pharmacology
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Dopamine Antagonists / chemical synthesis
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Dopamine Antagonists / chemistry*
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Dopamine Antagonists / pharmacology
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Dopamine D2 Receptor Antagonists
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Drug Design
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Humans
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Neurotransmitter Agents / chemical synthesis
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Neurotransmitter Agents / chemistry*
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Neurotransmitter Agents / pharmacology
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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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Benzazepines
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Dopamine Antagonists
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Dopamine D2 Receptor Antagonists
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Neurotransmitter Agents
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Receptors, Dopamine D1
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Receptors, Dopamine D2
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SCH 23390
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Benzodiazepines