In Vivo Occupancy of Dopamine D3 Receptors by Antagonists Produces Neurochemical and Behavioral Effects of Potential Relevance to Attention-Deficit–Hyperactivity Disorder

@article{Barth2013InVO,
  title={In Vivo Occupancy of Dopamine D3 Receptors by Antagonists Produces Neurochemical and Behavioral Effects of Potential Relevance to Attention-Deficit–Hyperactivity Disorder},
  author={Vanessa N. Barth and Anne B. Need and Eleni T. Tzavara and Bruno Giros and Carl D. Overshiner and Scott D. Gleason and Mark R. Wade and Anette M. Johansson and Kenneth W. Perry and G. Nomikos and Jeffrey M. Witkin},
  journal={The Journal of Pharmacology and Experimental Therapeutics},
  year={2013},
  volume={344},
  pages={501 - 510}
}
  • V. Barth, A. Need, +8 authors J. Witkin
  • Published 1 February 2013
  • Biology, Psychology, Chemistry
  • The Journal of Pharmacology and Experimental Therapeutics
Dopamine D3 receptors have eluded definitive linkage to neurologic and psychiatric disorders since their cloning over 20 years ago. We report a new method that does not employ a radiolabel for simultaneously defining in vivo receptor occupancy of D3 and D2 receptors in rat brain after systemic dosing using the tracer epidepride (N-[[(2S)-1-ethylpyrrolidin-2-yl]methyl]-5-iodo-2,3-dimethoxybenzamide). Decreases in epidepride binding in lobule 9 of cerebellum (rich in D3 receptors) were compared… 
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An overview and update of the major aspects of research related to D3Rs: distribution in the CNS and periphery, signaling and molecular properties, the status of ligands available for D3R research (agonists, antagonists and partial agonists), behavioral functions of D2Rs, the role in neural networks, and a summary on how the D2R-related drug research has been translated to human therapy are provided.
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Low dose pramipexole causes D3 receptor-independent reduction of locomotion and responding for a conditioned reinforcer
¹²⁴I-Epidepride: a PET radiotracer for extended imaging of dopamine D2/D3 receptors.
Imaging Alcohol Induced Dopamine Release in the Human Brain: a PET/[11C]-(+)-PHNO Study
TLDR
The alcohol-induced dopaminergic response in social drinkers using [C]-(+)-PHNO is explored, suggesting that this response may be heterogeneous and the various factors influencing this response warrant further investigation.
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