3466-75-9

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Dihydrotetrabenazine is an active metabolite of the vesicular monoamine transporter 2 (VMAT2) inhibitor tetrabenazine that is generated by hepatic carbonyl reductases. Dihydrotetrabenazine binds to mouse pons medulla, hypothalamus, and striatum (K_ds = 2.72, 2.28, and 2.4 nM, respectively) and inhibits synaptic vesicular serotonin (5-HT) uptake (IC₅₀s = 2.2, 2.8, and 2.3 nM, respectively). It also binds to human caudate nucleus, hippocampus, and substantia nigra pars compacta (K_ds = 2.9, 2.5, and 2.8 nM, respectively). Dihydrotetrabenazine stereoisomers bind to VMAT2 in rat striatum.

Dihydrotetrabenazine (DHTBZ) is the active metabolite of Tetrabenazine (HY-B0590). Dihydrotetrabenazine is the inhibitor for human vesicular monoamine transporter 2 (VMAT2), that reduces monoamine content in presynaptic neurons, and can be used in movement disorder research[1].

ChEBI: B-Dihydrotetrabenazine is a member of isoquinolines.

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[1] Chen JJ, et al., Tetrabenazine for the treatment of hyperkinetic movement disorders: a review of the literature. Clin Ther. 2012 Jul;34(7):1487-504. DOI:10.1016/j.clinthera.2012.06.010