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Selective Dopamine D3 Receptor Antagonists: A Review 2001-2005

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A growing body of evidence indicates that dopamine (DA) D3 receptors are significantly involved in the control of drug-seeking behavior, and may play an important role in the pathophysiology of impulse control disorders and schizophrenia. This hypothesis has been difficult to test due to the lack of compounds with high selectivity for central DA D3 receptors. Recently, however, the synthesis and characterization of new highly potent and selective DA D3 receptor antagonists has permitted to characterize the role of the DA D3 receptor in a wide range of preclinical animal models. Although the proof of efficacy of pharmacotherapeutic agents is to be derived ultimately from clinical trials, the preclinical findings that selective antagonism at DA D3 receptors reduces the reinforcing efficacy of drugs of abuse, reverses cognitive deficits, and shows efficacy in animal models of schizophrenia add to an accumulating body of evidence that selective DA D3 receptor antagonists may hold highest promise in the treatment of several neuropsychiatric diseases. The present review is aiming at describing current areas of interest and the possible future development of selective DA D3 receptor antagonists by outlining about 40 patents and 100 publications in this research field between 2001 and 2005.

Keywords: Dopamine receptor; addiction; cognition; impulsivity; schizophrenia

Document Type: Research Article


Affiliations: Centre of Excellence for Drug Discovery in Psychiatry, Department of Biology, GlaxoSmithKline S.p.A.,Via A. Fleming 4, 37135 Verona, Italy.

Publication date: November 1, 2006

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  • Recent Patents on CNS Drug Discovery publishes review articles on recent patents in the field of CNS drug discovery e.g. novel bioactive compounds, analogs & targets. A selection of important and recent patents on CNS drug discovery is also included in the journal. The journal is essential reading for all researchers involved in CNS drug design and discovery.

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