Distinct cortical and striatal actions of a β-arrestin-biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties.

@article{Urs2016DistinctCA,
  title={Distinct cortical and striatal actions of a β-arrestin-biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties.},
  author={Nikhil M Urs and Steven M. Gee and Thomas F. Pack and John D. McCorvy and Tama Evron and Joshua C. Snyder and Xiaobao Yang and Ramona Marie Rodriguiz and Emiliana Borrelli and William C. Wetsel and Jian Jin and Bryan L. Roth and Patricio O'Donnell and Marc G. Caron},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={2016},
  volume={113 50},
  pages={E8178-E8186}
}
The current dopamine (DA) hypothesis of schizophrenia postulates striatal hyperdopaminergia and cortical hypodopaminergia. Although partial agonists at DA D2 receptors (D2Rs), like aripiprazole, were developed to simultaneously target both phenomena, they do not effectively improve cortical dysfunction. In this study, we investigate the potential for newly developed β-arrestin2 (βarr2)-biased D2R partial agonists to simultaneously target hyper- and hypodopaminergia. Using neuron-specific βarr2… CONTINUE READING
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