ML417 是选择性的，可透过血脑屏障的 D3 多巴胺受体激动剂，EC50=38 nM。它能够促进 D3R 介导的 β-arrestin 易位、G 蛋白介导的信号传导和 PERK 磷酸化，对其他 GPCR 介导的信号传导影响最小。它对毒素诱导的多巴胺能神经元变性具有神经保护活性。

ML417 is a selective and brain penetrant agonist of D3 Dopamine (EC50 : 38 nM).

Molecular modeling suggests that ML417 interacts with the D3R in a unique manner, possibly explaining its remarkable selectivity.?ML417 was also found to protect against neurodegeneration of dopaminergic neurons derived from iPSCs.?Together with promising pharmacokinetics and toxicology profiles, these results suggest that ML417 is a novel and uniquely selective D3R agonist that may serve as both a research tool and a therapeutic lead for the treatment of neuropsychiatric disorders.

1386162-69-1

C22H25N3O3

379.46

DMSO:50 mg/mL (131.77 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years