Communication

Tritium-Labeled Brivaracetam with High Specific Activity: Preparation, Characterization and Application in Human Brain Samples

  1. Simone Hildenbrand1,
  2. Prof. Dr. Susanne Schoch2,
  3. Dr. Marec von Lehe2,
  4. Dr. Rainer Surges2,
  5. Prof. Dr. Christa E. Müller1,*

Article first published online: 27 JUN 2012

DOI: 10.1002/cmdc.201200183

Issue

ChemMedChem

ChemMedChem

Volume 7, Issue 8, pages 1369–1374, August 2012

Additional Information

How to Cite

Hildenbrand, S., Schoch, S., von Lehe, M., Surges, R. and Müller, C. E. (2012), Tritium-Labeled Brivaracetam with High Specific Activity: Preparation, Characterization and Application in Human Brain Samples. ChemMedChem, 7: 1369–1374. doi: 10.1002/cmdc.201200183

Author Information

  1. 1

    Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, 53121 Bonn (Germany)

  2. 2

    Departments of Neuropathology, Neurosurgery and Epileptology, University of Bonn Medical Center, Sigmund-Freud Str. 25, 53127 Bonn (Germany)

*Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, 53121 Bonn (Germany)

Publication History

  1. Issue published online: 31 JUL 2012
  2. Article first published online: 27 JUN 2012
  3. Manuscript Revised: 9 JUN 2012
  4. Manuscript Received: 3 APR 2012

Funded by

  • International Isotope Society—Central European Division (IIS-CED)
  • German Federal Ministry for Education and Research (BMBF). Grant Number: NGFNplus-EMINET
  • Deutsche Forschungsgemeinschaft (DFG). Grant Numbers: Graduiertenkolleg 804, SFB/TR3, SFB-645
  • University of Bonn BONFOR Research Program

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Keywords:

  • binding assays;
  • epilepsy;
  • isotopic labeling;
  • radioligands;
  • radiopharmaceuticals;
  • synaptic vesicle glycoprotein 2A (SV2A)
Thumbnail image of graphical abstract

Fine tuning the radio: A novel synthetic route to tritium-labeled brivaracetam ([3H]BRV) provided the radioligand with high specific activity (94 Ci mmol−1, 3.5 TBq mmol−1). [3H]BRV represents a powerful tool for the labeling of high-affinity binding sites of this antiepileptic drug, with potential application in the screening of compound libraries.

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