ML-417

ML-417 is a dopamine D₃ receptor agonist.¹ It is selective for the dopamine D₃ receptor over the dopamine D₂ receptor (EC₅₀s = 38 and >10,000 nM, respectively, in β-arrestin recruitment assays using CHO-K1 cells expressing the human receptors) and dopamine D₁, D₄, and D₅ receptors, as well as a panel of 45 G protein-coupled receptors (GPCRs), transporters, and ion channels at 10 µM. ML-417 inhibits forskolin-induced cAMP accumulation in HEK293 cells expressing the human dopamine D₃ receptor (IC₅₀ = 86 nM) and induces phosphorylation of ERK in CHO-K1 cells expressing the human dopamine D₃ receptor (EC₅₀ = 21 nM). It protects against cell death induced by the catecholaminergic neurotoxin 6-OHDA (Item No. 25330) in human induced pluripotent stem cell-derived (iPSC-derived) cells differentiated into dopaminergic neurons when used at a concentration of 50 nM.

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1. Moritz, A.E., Free, R.B., Weiner, W.S., et al. Discovery, optimization, and characterization of ML417: A novel and highly selective D₃ dopamine receptor agonist. J. Med. Chem. 63(10), 5526-5567 (2020).