ACP-103, a 5-Hydroxytryptamine 2A Receptor Inverse Agonist, Improves the Antipsychotic Efficacy and Side-Effect Profile of Haloperidol and Risperidone in Experimental Models

  title={ACP-103, a 5-Hydroxytryptamine 2A Receptor Inverse Agonist, Improves the Antipsychotic Efficacy and Side-Effect Profile of Haloperidol and Risperidone in Experimental Models},
  author={Luis R. Gardell and Kimberly E. Vanover and Linda Pounds and Robert W. Johnson and Richard A. Barido and Gary Anderson and Isaac Veinbergs and Agnete Dyssegaard and Per Brunmark and Ali Reza Tabatabaei and Robert E Davis and Mark R. Brann and Uli Hacksell and Douglas W Bonhaus},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={862 - 870}
Dopamine D2 receptor antagonism contributes to the therapeutic action of antipsychotic drugs (APDs) but also produces undesirable side effects, including extrapyramidal motor deficits, cognitive dulling, and prolactinemia. The introduction of atypical APDs was a significant advancement in the treatment of schizophrenia. Whereas these agents are D2 receptor antagonists, they are also potent 5-hydroxytryptamine (5-HT)2A receptor inverse agonists, a feature that may explain their improved efficacy… 

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