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Since its discovery, the dopamine D3 receptor has become an important therapeutic target for the development of drugs for neuropsychiatric disorders and Parkinson’s disease. Consequently, an enormous amount of effort has been directed towards development of D3 receptor‐selective molecules. Here we present a comprehensive review on drug development directed towards D3 receptors for the treatment of Parkinson’s disease. D3 receptor‐selective molecules belonging to both agonist and antagonist classes are included. Furthermore, the potential of D3 receptors as neuroprotective targets, as well as their role in the development and treatment of L‐DOPA‐induced dyskinesia, is also covered.

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