Intrinsic Efficacy of Antipsychotics at Human D2, D3, and D4 Dopamine Receptors: Identification of the Clozapine Metabolite N-Desmethylclozapine as a D2/D3 Partial Agonist

  title={Intrinsic Efficacy of Antipsychotics at Human D2, D3, and D4 Dopamine Receptors: Identification of the Clozapine Metabolite N-Desmethylclozapine as a D2/D3 Partial Agonist},
  author={Ethan S. Burstein and J X Ma and S. Wong and Y Gao and E. Pham and Anne Eeg Knapp and Norman R. Nash and Roger Olsson and R. E. Davis and Uli Hacksell and David M Weiner and Mark R. Brann},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={1278 - 1287}
  • E. Burstein, J. Ma, M. Brann
  • Published 1 December 2005
  • Psychology, Medicine
  • Journal of Pharmacology and Experimental Therapeutics
Drugs that antagonize D2-like receptors are effective antipsychotics, but the debilitating movement disorder side effects associated with these drugs cannot be dissociated from dopamine receptor blockade. The “atypical” antipsychotics have a lower propensity to cause extrapyramidal symptoms (EPS), but the molecular basis for this is not fully understood nor is the impact of inverse agonism upon their clinical properties. Using a cell-based functional assay, we demonstrate that overexpression of… 

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