ML417 is a blood-brain barrier permeable, potent and highly selective agonist of D3 dopamine receptor (D3R) with very limited cross-reactivity at other GPCRs. ML417 potently induces G-protein activation, D3R-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.
blood-brain barrier permeable, potent and highly selective agonist of D3 dopamine receptor (D3R)
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
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Journal of medicinal chemistry, 63(10), 5526-5567 (2020-04-29)
To identify novel D3 dopamine receptor (D3R) agonists, we conducted a high-throughput screen using a β-arrestin recruitment assay. Counterscreening of the hit compounds provided an assessment of their selectivity, efficacy, and potency. The most promising scaffold was optimized through medicinal
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