title: Monitoring of serum bioactivity levels of perazine and its metabolites by radioreceptor assay.
abstract: The bioactivity of perazine and its metabolites in human serum was analysed by radioreceptor assay. The IC50 value (the concentration eliciting a 50% blockade of 3H-spiroperidol binding to the dopamine receptor in a membrane suspension of porcine striatum) was for perazine 175 nmol/l, and for its metabolites perazine sulfoxide 1050 nmol/l, desmethylperazine 330 nmol/l, N-(3-phenothiazin-10-yl-propyl)-ethylenediamine 2800 nmol/l, and N-(3-phenothiazin-10-yl-propyl)-N'-methylethylenediamin 2850 nmol/l. Thus, perazine metabolites possess low affinity to the dopamine receptor. In a pilot study we measured the bioactivity of perazine and its metabolites in sera of perazine-treated psychiatric patients by radioreceptor assay and compared the results to levels obtained by high-performance thin-layer chromatography; the correlation coefficient r was 0.85 and the slope 0.95 (n = 11). Thus serum perazine can be adequately monitored by radioreceptor assay, as evidenced by the results from high-performance thin-layer chromatography.
authors.affiliation: Department of Psychiatry, University of Bonn, FRG.
authors.forename: M L
authors.initials: ML
authors.lastname: Rao
mesh_terms: D000293:Adolescent; D000328:Adult; D000368:Aged; D014150:Antipsychotic Agents / Q000097:blood*; D001667:Binding, Competitive / Q000187:drug effects; D002746:Chlorpromazine / Q000494:pharmacology; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D008991:Monitoring, Physiologic; D010464:Perazine / Q000097:blood*; D011869:Radioligand Assay; D011954:Receptors, Dopamine / Q000187:drug effects / Q000378:metabolism; D013134:Spiperone / Q000378:metabolism
chemical_list: D014150:Antipsychotic Agents; D011954:Receptors, Dopamine; D013134:Spiperone; D010464:Perazine; D002746:Chlorpromazine