Antipsychotic agents differ in how fast they come off the dopamine D2 receptors. Implications for atypical antipsychotic action.

@article{Kapur2000AntipsychoticAD,
  title={Antipsychotic agents differ in how fast they come off the dopamine D2 receptors. Implications for atypical antipsychotic action.},
  author={Shitij Kapur and Philip Seeman},
  journal={Journal of psychiatry & neuroscience : JPN},
  year={2000},
  volume={25 2},
  pages={161-6}
}
RATIONALE AND OBJECTIVE While the blockade of dopamine D2 receptors are necessary for antipsychotic action, antipsychotic agents differ nearly a thousand-fold in their affinity for the D2 receptor. This affinity is determined by the rate at which the antipsychotic agent binds to (kon) and the rate at which it dissociates from (koff) the D2 receptors. The objective of this study was to determine the relationship between kon, koff and the affinity (Ki) of antipsychotic agents for the D2 receptors… CONTINUE READING
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