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Dopamine D3 receptor agonist 13a is a dopamine D3 receptor agonist.1 It selectively binds to dopamine D3 over dopamine D1, D2, and D4 receptors (Kis = 0.14, 4,600, 2.85, and 756 nM, respectively), as well as the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT2A, 5-HT2B, and 5-HT2C (Kis = 6, 54, 1.47, and 252 nM, respectively), however, it is a partial agonist of dopamine D2 receptors (EC50 = 2.26 nM in a G protein recruitment assay) and acts as an antagonist at dopamine D3 receptors (IC50 = 4.62 nM). Dopamine D3 receptor agonist 13a (3 mg/kg) reduces cocaine self-administration in rats.
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1. Dopamine D3/D2 receptor ligands based on cariprazine for the treatment of psychostimulant use disorders that may be dual diagnosed with affective disorders. J. Med. Chem. 66(3), 1809-1834 (2023).