Selective dopamine D₃receptor antagonists. A decade of progress: 1997 – 2007

This is the authors' abstract. We don't add key points for this paper.

Background: A growing number of patent applications on dopamine (DA) D3 receptors have been filed over the last 10 years. The increased interest in this target correlates with evidence that implicates the DA D3 receptor in the control of drug-seeking behavior and in the pathophysiology of some impulse control disorders and schizophrenia. Objectives: This manuscript provides an overview of the most recent literature in support of the biologic rationale for the use of selective DA D3 receptor antagonists for neuropsychiatric indications, and reviews > 80 patents that reflect 10-year advances in the discovery of these compounds by pharmaceutical companies, national research institutes and academic groups. Methods: Analysis of > 100 primary literature and 80 patent references of the last 10 years. Conclusions: The recent synthesis and profiling of new highly potent and selective DA D3 receptor antagonists over the last 10 years has permitted the testing of these compounds in a wide range of preclinical animal models of neuropsychiatric diseases. Clinical trials have now been initiated and clinical proof-of-concept is expected in the forthcoming years.