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

@article{Burstein2005IntrinsicEO,
  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={E. Burstein and J. Ma and S. Wong and Y. Gao and E. Pham and A. E. Knapp and N. Nash and R. Olsson and R. Davis and U. Hacksell and D. Weiner and M. Brann},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2005},
  volume={315},
  pages={1278 - 1287}
}
  • E. Burstein, J. Ma, +9 authors M. Brann
  • Published 2005
  • Chemistry, 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… CONTINUE READING
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