Dihydrotetrabenazine Explained

Dihydrotetrabenazine or DTBZ is an organic compound with the chemical formula C19H29NO3. It is a close analog of tetrabenazine. DTBZ and its derivatives, when labeled with positron emitting isotopes such as carbon-11 and fluorine-18, are used as PET radioligands for examining VMAT2.[1]

Use in Positron Emission Tomography

[<sup>11</sup>C]DTBZ as a PET radioligand with affinity for VMAT2 was developed in the mid 1990s by David E. Kuhl and colleagues at the University of Michigan.[2] There are two enantiomers of alpha-dihydrotetrabenazine, and the dextrorotary(or (+) isomer) has a high affinity of about 1 nanomolar Ki whereas the levorotary (or (-) isomer) has approximately 1000 fold lower affinity with a Ki of about 2 micromolar.[3]

VMAT2 is a membrane bound protein and a biomarker for Parkinson's disease. Binding of DTBZ to VMAT2 in individuals with Parkinson's disease is significantly reduced.[4] Moreover, the VMAT2 density as determined by [<sup>18</sup>F]DTBZ has been shown to be well, inversely correlated with the severity of Parkinson's disease.[5]

Avid Radiopharmaceuticals has sponsored clinical trials of [<sup>18</sup>F]AV-133 (or [<sup>18</sup>F]Fluoropropyl-(+)-DTBZ) to identify subjects with dopaminergic degeneration.[6]

See also

Notes and References

  1. Koeppe. RA. Gilman. S. Joshi. A. Liu. S. Little. R. Junck. L. Heumann. M. Frey. KA. Albin. RL. 11C-DTBZ and 18F-FDG PET measures in differentiating dementias.. Journal of Nuclear Medicine . June 2005. 46. 6. 936–44. 15937303.
  2. Frey. KA. Koeppe. RA. Kilbourn. MR. Vander Borght. TM. Albin. RL. Gilman. S. Kuhl. DE. Presynaptic monoaminergic vesicles in Parkinson's disease and normal aging.. Annals of Neurology. December 1996. 40. 6. 873–84. 9007092. 10.1002/ana.410400609. 2027.42/50362. 9419161. free.
  3. Kilbourn. M. Lee. L. Vander Borght. T. Jewett. D. Frey. K. Binding of alpha-dihydrotetrabenazine to the vesicular monoamine transporter is stereospecific.. European Journal of Pharmacology. 24 May 1995. 278. 3. 249–52. 7589162. 10.1016/0014-2999(95)00162-e.
  4. Wang. Jian. Hoekstra. Jake G.. Zuo. Chuantao. Cook. Travis J.. Zhang. Jing. Biomarkers of Parkinson's disease: current status and future perspectives. Drug Discovery Today. February 2013. 18. 3–4. 155–162. 10.1016/j.drudis.2012.09.001. 3557745. 22982303.
  5. Hsiao. Ing-Tsung. Weng. Yi-Hsin. Hsieh. Chia-Ju. Lin. Wey-Yil. Wey. Shiaw-Pyng. Kung. Mei-Ping. Yen. Tzu-Chen. Lu. Chin-Song. Lin. Kun-Ju. Correlation of Parkinson Disease Severity and F-DTBZ Positron Emission Tomography. JAMA Neurology. 1 June 2014. 71. 6. 758–766. 10.1001/jamaneurol.2014.290. 24756323.
  6. Web site: A Trial of 18F-AV-133 Positron Emission Tomography (PET) Imaging to Differentiate Subjects With Parkinson's Disease (PD) From Other Movement Disorders. Clinical Trials. U.S. National Institutes of Health. 20 July 2015.

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