Drug intelligence / Profile preview

(-)-[11C]dihydrotetrabenazine

Development stage
Preclinical
Lead developer
University of Michigan
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

(-)-[11C]dihydrotetrabenazine ((-)-[11C]DTBZ) is a radiolabeled small molecule used as a positron emission tomography (PET) imaging research tool. It is the levorotary stereoisomer of dihydrotetrabenazine, labeled with the positron-emitting isotope carbon-11. While its structural target is the vesicular monoamine transporter type 2 (VMAT2), the (-)-isomer possesses an extremely low affinity for this transporter (Ki ≈ 2.2 μmol/L) compared to its (+)-enantiomer (Ki ≈ 1 nmol/L). Due to this low affinity, it is primarily utilized in clinical research as an inactive control to quantify and subtract nonspecific binding and free tracer signal, thereby allowing for more precise determination of specific VMAT2 binding when used alongside the active (+)-isomer. It was developed at the University of Michigan and is used to study neurological conditions such as Parkinson's disease and Tourette syndrome.

Other names
(-)-alpha-[11C]dihydrotetrabenazine(-)-9,10-dimethoxy-3-(2-methylpropyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol
02

Targets

VMAT2 (Vesicular monoamine transporter 2)

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