Aripiprazole, a Novel Antipsychotic, Is a High-Affinity Partial Agonist at Human Dopamine D2 Receptors

  title={Aripiprazole, a Novel Antipsychotic, Is a High-Affinity Partial Agonist at Human Dopamine D2 Receptors},
  author={Kevin D. Burris and Thaddeus F. P. Molski and Cen Xu and Elaine Ryan and Katsura Tottori and Tetsuro Kikuchi and Frank D. Yocca and Perry B. Molinoff},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={381 - 389}
  • K. Burris, T. Molski, P. Molinoff
  • Published 1 July 2002
  • Psychology, Biology, Chemistry
  • Journal of Pharmacology and Experimental Therapeutics
Aripiprazole is the first next-generation atypical antipsychotic with a mechanism of action that differs from currently marketed typical and atypical antipsychotics. Aripiprazole displays properties of an agonist and antagonist in animal models of dopaminergic hypoactivity and hyperactivity, respectively. This study examined the interactions of aripiprazole with a single population of human D2 receptors to clarify further its pharmacologic properties. In membranes prepared from Chinese hamster… 

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