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Carbon-11 Choline: Synthesis, Purification, and Brain Uptake Inhibition by 2-Dimethylaminoethanol

Donner Laboratory, Lawrence Berkeley Laboratory, University of California, Berkeley, California

Correspondence: For reprints contact: Mark A. Rosen, MD, Donner Laboratory, Lawrence Berkeley Laboratory, University of California, Berkeley, CA 94720.

ABSTRACT

We report an improved method for the synthesis and purification of [¹¹C]methylcholine from the precursors [¹¹C]methyliodide and 2-dimethylaminoethanol (deanol). Preparation time, including purification, is 35 min postbombardment. Forty millicuries of purified injectable [¹¹C]choline were produced with a measured specific activity of >300 Ci/mmol and a radiochemical purity >98%. The decay corrected radiochemical yield for the synthesis and purification was 50%. Residual precursor deanol, which inhibits brain uptake of choline, is removed by a rapid preparative high performance liquid chromatography (HPLC) method using a reverse phase cyano column with a biologically compatible 100% water eluent. Evaporation alone did not completely remove the deanol precursor. Brain uptake of the [¹¹C]choline product was six times greater after HPLC removal of deanol because doses of less than 1 µg/kg significantly inhibit [¹⁴C]choline brain uptake.

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