Document Detail

Dopamine D3 receptor antagonists: a patent review (2007 - 2012).
MedLine Citation:
PMID:  23282131     Owner:  NLM     Status:  MEDLINE    
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.
Fabrizio Micheli; Christian Heidbreder
Publication Detail:
Type:  Journal Article; Review     Date:  2013-01-03
Journal Detail:
Title:  Expert opinion on therapeutic patents     Volume:  23     ISSN:  1744-7674     ISO Abbreviation:  Expert Opin Ther Pat     Publication Date:  2013 Mar 
Date Detail:
Created Date:  2013-02-15     Completed Date:  2013-08-09     Revised Date:  2014-03-25    
Medline Journal Info:
Nlm Unique ID:  9516419     Medline TA:  Expert Opin Ther Pat     Country:  England    
Other Details:
Languages:  eng     Pagination:  363-81     Citation Subset:  IM    
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MeSH Terms
Antiparkinson Agents / pharmacology
Clinical Trials as Topic
Cognition / drug effects
Dopamine Antagonists / pharmacology*,  therapeutic use
Ejaculation / drug effects
Impulse Control Disorders / drug therapy,  psychology
Kidney Diseases / prevention & control
Limbic System / drug effects,  physiology
Motivation / drug effects
Patents as Topic
Randomized Controlled Trials as Topic
Receptors, Dopamine D3 / antagonists & inhibitors*
Recurrence / prevention & control
Schizophrenia / drug therapy
Substance-Related Disorders / drug therapy,  psychology
Reg. No./Substance:
0/Antiparkinson Agents; 0/Dopamine Antagonists; 0/Receptors, Dopamine D3

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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