- Pharmacologic Characterization of Valbenazine (NBI-98854) and Its Metabolites.
Pharmacologic Characterization of Valbenazine (NBI-98854) and Its Metabolites.
The Journal of pharmacology and experimental therapeutics (2017-04-14)
Dimitri E Grigoriadis, Evan Smith, Sam R J Hoare, Ajay Madan, Haig Bozigian
PMID28404690
摘要
The vesicular monoamine transporter 2 (VMAT2) is an integral presynaptic protein that regulates the packaging and subsequent release of dopamine and other monoamines from neuronal vesicles into the synapse. Valbenazine (NBI-98854), a novel compound that selectively inhibits VMAT2, is approved for the treatment of tardive dyskinesia. Valbenazine is converted to two significant circulating metabolites in vivo, namely, (+)-