ML417 (ML 417) is a novel potent and uniquely selective D3 dopamine receptor (D3R) full agonist with EC50 of 38 nM in β-arrestin recruitment assays. ML417 displays global selectivity at all other receptor subtypes, very limited activity (IC50 > 50 uM) at all subtypes except for the D2R, exhibits submicromolar affinity for only 3 targets, the β1-adrenergic, 5-HT2B, and σ-1 receptor in large arrays of GPCRs and several transporters or ion channels.
ML417 potently promotes D3R-mediated β-arrestin translocation, G protein activation, and ERK1/2 phosphorylation (pERK) while lacking activity at other dopamine receptors.
ML417 protect D3R-expressing dopaminergic neurons from 6-OHDA-induced cell death.
