Abstract
A new diaryl-methylene piperidine derivative, 2, displayed an atypical antipsychotic profile both in vitro and in vivo. The main pharmacological characteristics of this compound appears to reside in a more potent antagonism of the 5-HT2 serotonergic receptor than of the D2 dopaminergic receptor. This confirms that molecules displaying a D2/5-HT2 binding ratio < 1 possess clozapine-like antipsychotic activity.
MeSH terms
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Animals
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Antipsychotic Agents / chemical synthesis*
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Antipsychotic Agents / metabolism
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Antipsychotic Agents / pharmacology
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Antipsychotic Agents / toxicity
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Disease Models, Animal
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Dose-Response Relationship, Drug
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Drug Evaluation, Preclinical
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Mice
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Piperidines / chemical synthesis
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Piperidines / metabolism
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Piperidines / pharmacology*
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Protein Binding
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Psychomotor Agitation / drug therapy
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Psychotic Disorders / drug therapy
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Receptors, Dopamine D2 / metabolism
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Receptors, Serotonin / metabolism
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Serotonin Antagonists / chemical synthesis
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Serotonin Antagonists / metabolism
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Serotonin Antagonists / pharmacology
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Serotonin Antagonists / toxicity
Substances
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Antipsychotic Agents
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Piperidines
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Receptors, Dopamine D2
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Receptors, Serotonin
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Serotonin Antagonists