Synthesis of ~3H-labeled Tetrabenazine (TBZ)

摘要

Tetrabenazine (TBZ), which was introduced in 1956 as an antipsychotic drug, is currently used as treatment for hyperkinetic movement disorders. TBZ is considered a classical inhibitor of vesicular monamine transporter 2 (VMAT2). VMAT2 is the only transport that moves cytoplasmic dopamine into synaptic vesicles for storage and subsequent release in the central nervous system.5 It has been shown to deplete cerebral monoamines in rat brain by reversibly inhibiting VMAT2. TBZ (Xenazine~R) is approved by the U.S. Food and Drug Administration (FDA) to treat chorea, the jerky, involuntary movement, that occurs in people with Huntington's disorder. It is also used to alleviate tics in Tourette's syndrome and movement disorders in tardive dyskinesia.