Display options
Share it on

Eur J Med Chem. 2021 Nov 15;224:113718. doi: 10.1016/j.ejmech.2021.113718. Epub 2021 Jul 24.

Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.

European journal of medicinal chemistry

Yifei Yang, Dawei Yu, Xiaoyin Zhu, Guangying Du, Wenyan Wang, Fangxia Zou, Hongbo Wang, Rui Zhang, Liang Ye, Jingwei Tian

Affiliations

  1. School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai, 264005, China.
  2. Medicinal Chemistry Research Department, R & D Center (Luye Pharma Group Ltd.), Yantai, 264003, PR China.
  3. Medicinal Chemistry Research Department, R & D Center (Luye Pharma Group Ltd.), Yantai, 264003, PR China. Electronic address: [email protected].
  4. Department of Clinical Medicine, Binzhou Medical College, Yantai, 256603, China. Electronic address: [email protected].
  5. School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai, 264005, China. Electronic address: [email protected].

PMID: 34329999 DOI: 10.1016/j.ejmech.2021.113718

Abstract

Vesicular monoamine transporter 2 (VMAT2) is essential for synaptic transmission of all biogenic amines in the brain including serotonin, norepinephrine, histamine, and dopamine (DA). Given its crucial role in the neurophysiology and pharmacology of the central nervous system, VMAT2 is recognized as an important therapeutic target for various neurological disorders such as tardive dyskinesia (TD). Here, a novel series of dihydrotetrabenazine derivative analogs were designed and synthesized to evaluate their effects on [

Copyright © 2021 Elsevier Masson SAS. All rights reserved.

Keywords: DA uptake; Dihydrotetrabenazine; Tardive dyskinesia; Vesicular monoamine transporter 2

Conflict of interest statement

Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this pa

Publication Types