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Valbenazine is an inhibitor of vesicular monoamine transporter 2 (VMAT2; Kis = 110 and 150 nM in rat striatum homogenates and human platelets, respectively).1 It is selective for VMAT2 over a panel of 80 receptors, transporters, and ion channels, including the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT2A, and 5-HT2B and dopamine D1 and D2 receptors. Valbenazine induces ptosis in rats, indicating norepinephrine depletion. Formulations containing valbenazine have been used in the treatment of tardive dyskinesia.
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1. Pharmacologic characterization of valbenazine (NBI-