Hybridization of amantadine with gardenamide A enhances NMDA antagonism and in vivo anti-PD effects

Wenda Zhu,Yiping Fan,Yanbing Li,Lizhi Peng,Yifang Li,Fengxia Yan,Jiaqiang Zhao,Lei Zhang,Hiroshi Kurihara,Rongrong He,Heru Chen

Bioorganic Chemistry（2023）

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摘要

•5b, the shortest conjugate of ATD/GA, is 4-fold more active than ATD.•5b showed better in vivo activity on reversing the damages of behavioral performance than ATD.•5b showed better in vivo activity on reversing the loss of dopaminergic neurons than ATD.•5b showed better in vivo activity on modulating Akt than ATD.

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关键词

Drug design,NMDAR antagonist,Parkinson’s disease,Neuroprotective agent,Dopaminergic neurons

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