1386162-69-1

ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons[1].

ML417 is a blood-brain barrier permeablepotent and highly selective agonist of D3 dopamine receptor (D3R) with very limited cross-reactivity at other GPCRs. ML417 potently induces G-protein activationD3R-mediated b-arrestin translocation and pERK phosphorylation. It does not activate other dopamine receptors. ML417 protect D3R-expressing dopaminergic neurons from 6-OHDA induced cell death.

D₃ Receptor: 38 nM (EC₅₀)

[1] Moritz AE, et al. Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D3 Dopamine Receptor Agonist. J Med Chem. 2020;63(10):5526‐5567. DOI:10.1021/acs.jmedchem.0c00424