(+)-9-Trifluoroethoxy-α-Dihydrotetrabenazine as a Highly Potent Vesicular Monoamine Transporter 2 Inhibitor for Tardive Dyskinesia

• Main Authors: Wenyan Wang (Author), Guangying Du (Author), Shilan Lin (Author), Jing Liu (Author), Huijie Yang (Author), Dawei Yu (Author), Liang Ye (Author), Fangxia Zou (Author), Hongbo Wang (Author), Rui Zhang (Author), Jingwei Tian (Author)
• Format: Book
• Published: Frontiers Media S.A., 2021-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Valbenazine and deutetrabenazine are the only two therapeutic drugs approved for tardive dyskinesia based on blocking the action of vesicular monoamine transporter 2 (VMAT2). But there exist demethylated inactive metabolism at the nine position for both them resulting in low availability, and CYP2D6...