Abstract
This paper describes the syntheses of several 1-aryl-4-(biarylmethylene)piperazines and the results of the determination of their affinity for D(2) and 5-HT(1A) receptors. A selection of these compounds was evaluated in vivo, resulting in the identification of a drug candidate which is being clinically evaluated as a potential atypical antipsychotic with reduced extrapyrimidal side effects.
MeSH terms
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8-Hydroxy-2-(di-n-propylamino)tetralin / metabolism
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8-Hydroxy-2-(di-n-propylamino)tetralin / pharmacology
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Animals
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Antipsychotic Agents / chemistry*
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Antipsychotic Agents / metabolism
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Antipsychotic Agents / pharmacology*
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Apomorphine / adverse effects
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Behavior, Animal / drug effects
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Benzoxazoles / chemistry*
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Benzoxazoles / metabolism
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Benzoxazoles / pharmacology*
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Dopamine Antagonists / metabolism
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Dopamine Antagonists / pharmacology
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Drug Design
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Drug Evaluation, Preclinical
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Mice
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Piperazines / chemistry*
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Piperazines / metabolism
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Piperazines / pharmacology*
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Rats
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Receptors, Dopamine D2 / drug effects
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Receptors, Dopamine D2 / metabolism*
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Receptors, Serotonin / drug effects
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Receptors, Serotonin / metabolism*
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Receptors, Serotonin, 5-HT1
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Serotonin Receptor Agonists / metabolism
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Serotonin Receptor Agonists / pharmacology
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Spiperone / metabolism
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Spiperone / pharmacology
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Structure-Activity Relationship
Substances
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7-(4-(3-phenylbenzyl)piperazin-1-yl)-1H-benzoxazol-2-one
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Antipsychotic Agents
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Benzoxazoles
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Dopamine Antagonists
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Piperazines
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Receptors, Dopamine D2
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Receptors, Serotonin
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Receptors, Serotonin, 5-HT1
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Serotonin Receptor Agonists
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Spiperone
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8-Hydroxy-2-(di-n-propylamino)tetralin
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Apomorphine