Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors

Atypical antipsychotics show reduced extrapyramidal side effects compared to first generation drugs. Here the authors use time-resolved FRET to measure binding kinetics, and show that side effects correlate with drug association rates to the D2 receptor, while dissociation rates correlate with prola...

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Bibliographic Details
Main Authors: David A. Sykes, Holly Moore, Lisa Stott, Nicholas Holliday, Jonathan A. Javitch, J. Robert Lane, Steven J. Charlton
Format: article
Language:EN
Published: Nature Portfolio 2017
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Q
Online Access:https://doaj.org/article/92ce2e6b0c464f92849b40c8f8648e24
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Summary:Atypical antipsychotics show reduced extrapyramidal side effects compared to first generation drugs. Here the authors use time-resolved FRET to measure binding kinetics, and show that side effects correlate with drug association rates to the D2 receptor, while dissociation rates correlate with prolactin elevation.