Nature Communications (Oct 2017)

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

  • David A. Sykes,
  • Holly Moore,
  • Lisa Stott,
  • Nicholas Holliday,
  • Jonathan A. Javitch,
  • J. Robert Lane,
  • Steven J. Charlton

DOI
https://doi.org/10.1038/s41467-017-00716-z
Journal volume & issue
Vol. 8, no. 1
pp. 1 – 11

Abstract

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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.