Abstract
The receptor binding profile of levomepromazine (LMP) in human brain was compared with that of clozapine (CLOZ) and chlorpromazine (CPZ). LMP showed significantly greater binding affinity for both alpha-1 and serotonin-2 binding sites than either CLOZ or CPZ, and significantly greater binding to alpha-2 sites than CPZ. A potent pharmacological effect at these receptor sites may explain the beneficial effect of LMP on psychotic symptoms and akathisia in treatment-resistant schizophrenia recently described in 2 open studies. LMP requires further appraisal as a potentially useful neuroleptic in the management of treatment-resistant schizophrenia.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adolescent
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Aged
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Binding, Competitive / physiology
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Brain / drug effects
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Brain / metabolism*
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Brain / pathology
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Chlorpromazine / pharmacokinetics
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Chlorpromazine / therapeutic use
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Clozapine / pharmacokinetics
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Clozapine / therapeutic use
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Corpus Striatum / metabolism
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Corpus Striatum / pathology
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Culture Techniques
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Female
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Frontal Lobe / metabolism
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Frontal Lobe / pathology
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Humans
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Male
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Methotrimeprazine / pharmacokinetics*
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Methotrimeprazine / therapeutic use
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Receptors, Dopamine / drug effects
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Receptors, Dopamine / metabolism*
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Receptors, Neurotransmitter / drug effects
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Receptors, Neurotransmitter / metabolism
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Schizophrenia / drug therapy
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Schizophrenia / metabolism*
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Schizophrenic Psychology*
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Synaptic Membranes / drug effects
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Synaptic Membranes / metabolism
Substances
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Receptors, Dopamine
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Receptors, Neurotransmitter
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phenothiazine receptor
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Methotrimeprazine
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Clozapine
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Chlorpromazine