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Antipsychotic radioreceptor assay: a modification identifying selective receptor effects
R A Sweet1, R A Henteleff, K A Meinert
1Geriatric Psychopharmacology Program, Division of Geriatrics and Neuropsychiatry, Department of Psychiatry, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania, USA. sweetra@msx.upmc.edu
Abstract:
Radioreceptor assays offer the advantage of a single assay that can assess uniform exposure to multiple chemical compounds. The advent of atypical antipsychotic agents has led to new awareness of the multiple receptor subtypes through which antipsychotic agents may exert their effects, and a renewed interest in comparative drug trials of antipsychotics. The objective of this study was to show the development and validation of antipsychotic radioreceptor assays using clonal cell lines stably expressing isolated human receptors. Model assays were developed using the dopamine(2) (D(2)) and D(4) receptors. D(2) and D(4) activities measured by radioreceptor assay in plasma of antipsychotic-treated subjects were highly correlated with high-performance liquid chromatography determinations of antipsychotic concentrations. Similarly, for a variety of typical and atypical antipsychotic agents, the quotients of D(4)/D(2) activity in plasma of antipsychotic-treated subjects were highly correlated with the quotients of D(4)/D(2) affinities of these agents. Valid receptor-selective antipsychotic assays can be established and may have utility for dissecting the in vivo activity of atypical antipsychotics in relation to specific outcomes in clinical trials.
Insights
Radioreceptor assays can now measure antipsychotic drug effects on dopamine receptors D(2) and D(4). These validated assays correlate well with drug levels and affinities, aiding clinical trial analysis.
Area of Science:
- Pharmacology
- Neuroscience
- Assay Development
Background:
- Atypical antipsychotics highlight the importance of multiple receptor subtypes in drug action.
- Comparative drug trials for antipsychotics require precise measurement of drug effects.
- Radioreceptor assays offer a method to assess exposure to multiple compounds simultaneously.
Purpose of the Study:
- To develop and validate radioreceptor assays for antipsychotics.
- To utilize clonal cell lines expressing human dopamine receptors D(2) and D(4).
- To assess the utility of these assays in understanding in vivo antipsychotic activity.
Main Methods:
- Development of model radioreceptor assays using dopamine D(2) and D(4) receptors.
- Stable expression of isolated human receptors in clonal cell lines.
- Measurement of receptor activity in plasma from antipsychotic-treated subjects.
Main Results:
- Radioreceptor assay measurements of D(2) and D(4) activity strongly correlated with HPLC-determined antipsychotic concentrations.
- Quotients of D(4)/D(2) activity in plasma correlated with D(4)/D(2) affinities for various antipsychotics.
- Validated receptor-selective antipsychotic assays were established.
Conclusions:
- Established radioreceptor assays are valid and useful for studying antipsychotic drug activity.
- These assays can help dissect the in vivo effects of atypical antipsychotics.
- The assays may aid in analyzing clinical trial outcomes related to specific receptor interactions.
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