Levomepromazine receptor binding profile in human brain--implications for treatment-resistant schizophrenia.
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.
McGill Center for Research in Schizophrenia, Douglas Hospital, Verdun, Quebec, Canada.
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D000293:Adolescent; D000368:Aged; D001667:Binding, Competitive / Q000502:physiology; D001921:Brain / Q000187:drug effects / Q000378:metabolism* / Q000473:pathology; D002746:Chlorpromazine / Q000493:pharmacokinetics / Q000627:therapeutic use; D003024:Clozapine / Q000493:pharmacokinetics / Q000627:therapeutic use; D003342:Corpus Striatum / Q000378:metabolism / Q000473:pathology; D046508:Culture Techniques; D005260:Female; D005625:Frontal Lobe / Q000378:metabolism / Q000473:pathology; D006801:Humans; D008297:Male; D008728:Methotrimeprazine / Q000493:pharmacokinetics* / Q000627:therapeutic use; D011954:Receptors, Dopamine / Q000187:drug effects / Q000378:metabolism*; D017981:Receptors, Neurotransmitter / Q000187:drug effects / Q000378:metabolism; D012559:Schizophrenia / Q000188:drug therapy / Q000378:metabolism*; D012565:Schizophrenic Psychology; D013570:Synaptic Membranes / Q000187:drug effects / Q000378:metabolism
D011954:Receptors, Dopamine; D017981:Receptors, Neurotransmitter; C028052:phenothiazine receptor; D008728:Methotrimeprazine; D003024:Clozapine; D002746:Chlorpromazine