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Dihydrotetrabenazine is a small molecule and the principal active metabolite of tetrabenazine, generated by hepatic metabolism. It acts as a potent inhibitor of vesicular monoamine transporter 2 (VMAT2), with high affinity for VMAT2 in the brain. The (+)-isomer is particularly active, exhibiting nanomolar affinity for VMAT2, while the (-)-isomer is much less active. Dihydrotetrabenazine and its radiolabeled derivatives are used as PET radioligands to image VMAT2 density in vivo, which serves as a biomarker for dopaminergic neuron integrity in disorders such as Parkinson's disease. It has also been investigated clinically for neurological disorders including tardive dyskinesia[1][5][10].
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