Dopamine D3 receptor ligand-5 (13a), a Cariprazine (HY-14763) analogue, is a dopamine D3 receptor ligand, with Ki values of 2.85 nM and 0.14 nM for D2R and D3R, respectively[1].
in vivo
Dopamine D3 receptor ligand-5 (13a) decreases cocaine self-administration (FR2; 1-10 mg/kg, i.p.) in rats, suggesting that partial agonists/antagonists with modest D3R/D2R-selectivity may be effective in treating PSUD and potentially comorbidities with other affective disorders[1].
[1] Emma S Gogarnoiu, et al. 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. 2023 Feb 9;66(3):1809-1834. DOI:10.1021/acs.jmedchem.2c01624
