Simple, rapid and reliable preparation of [¹¹C]-(+)-α-DTBZ of high quality for routine applications

Molecules. 2012 Jun 1;17(6):6697-704. doi: 10.3390/molecules17066697.

Abstract

[¹¹C]-(+)-α-DTBZ has been used as a marker of dopaminergic terminal densities in human striatum and expressed in islet beta cells in the pancreas. We aimed to establish a fully automated and simple procedure for the synthesis of [¹¹C]-(+)-α-DTBZ for routine applications. [¹¹C]-(+)-α-DTBZ was synthesized from a 9-hydroxy precursor in acetone and potassium hydroxide with [¹¹C]-methyl triflate and was purified by solid phase extraction using a Vac tC-18 cartridge. Radiochemical yields based on [¹¹C]-methyl triflate (corrected for decay) were 82.3% ± 3.6%, with a specific radioactivity of 60 GBq/μmol. Time elapsed was less than 20 min from end of bombardment to release of the product for quality control.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Carbon Radioisotopes
  • Mice
  • Quality Control
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / isolation & purification
  • Radiopharmaceuticals / pharmacokinetics
  • Tetrabenazine / analogs & derivatives*
  • Tetrabenazine / chemical synthesis
  • Tetrabenazine / isolation & purification
  • Tissue Distribution

Substances

  • (11C)-(+)-alpha-dihydrotetrabenazine
  • Carbon Radioisotopes
  • Radiopharmaceuticals
  • Tetrabenazine