Addiction Rehab: Dopamine D3 Receptor Antagonists: A Patent Review (2007 – 2012).

Dopamine D3 receptor antagonists: a patent review (2007 – 2012).

Filed under: Addiction Rehab

Expert Opin Ther Pat. 2013 Jan 3;
Micheli F, Heidbreder C

Introduction: The synthesis and characterization of new highly potent and selective dopamine (DA) D3 receptor antagonists has permitted to characterize the role of the DA D3 receptor in the control of drug-seeking behavior and in the pathophysiology of impulse control disorders and schizophrenia. Areas covered: In the present review, the authors will first describe most recent classes of DA D3 receptor antagonists by reviewing about 43 patent applications during the 2007 – 2012 period; they will then outline the biological rationale in support of the use of selective DA D3 receptor antagonists in the treatment of drug addiction, impulse control disorders and schizophrenia. Expert opinion: The strongest clinical application and potential for selective DA D3 receptor antagonists lies in the reduction of drug-induced incentive motivation, the attenuation of drug’s rewarding efficacy and the reduction in reinstatement of drug-seeking behavior triggered either by re-exposure to the drug itself, re-exposure to environmental cues that had been previously associated with drug-taking behavior or stress. The selectivity of these antagonists together with reduced lipophilicity (minimizing unspecific binding), increased brain penetration and improved physico-chemical profile are all key factors for clinical efficacy and safety.
HubMed – addiction


Repackaging cigarettes – will the courts thwart the FDA?

Filed under: Addiction Rehab

N Engl J Med. 2013 Jan 3; 368(1): 92

Repackaging Cigarettes – Will the Courts Thwart the FDA? Perspective, N Engl J Med 2012;367:2065-2067. In the first sentence of the article (page 2065), “August 12, 2012” should have been “August 15, 2012,” and “mouth ulcers” should have been “mouth cancer.” Also, in the reference list (page 2067), reference 5 should have been “Institute of Medicine. Ending the tobacco problem: a blueprint for the nation. Washington, DC: National Academies Press, 2007,” rather than “Institute of Medicine. Growing up tobacco free: preventing nicotine addiction in children and youths. Washington, DC: National Academies Press, 2007:237.” The article is correct at
HubMed – addiction



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