Carbon-11 choline: synthesis, purification, and brain uptake inhibition by 2-dimethylaminoethanol
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 greater than 300 Ci/mmol and a radiochemical purity greater than 98%. The decay corrected radiochemical yield for the synthesis and purification was approximately 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 microgram/kg significantly inhibit (14C)choline brain uptake.
- OSTI ID:
- 5750829
- Journal Information:
- J. Nucl. Med.; (United States), Vol. 12
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
62 RADIOLOGY AND NUCLEAR MEDICINE
CARBON 11
RADIOCHEMISTRY
RADIOPHARMACEUTICALS
CHEMICAL PREPARATION
PURIFICATION
BRAIN
CHOLINE
LABELLED COMPOUNDS
RATS
UPTAKE
ALCOHOLS
AMINES
AMMONIUM COMPOUNDS
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
CARBON ISOTOPES
CENTRAL NERVOUS SYSTEM
CHEMISTRY
DRUGS
EVEN-ODD NUCLEI
HYDROXY COMPOUNDS
ISOTOPES
LIGHT NUCLEI
LIPOTROPIC FACTORS
MAMMALS
MINUTES LIVING RADIOISOTOPES
NERVOUS SYSTEM
NUCLEI
ORGANIC COMPOUNDS
ORGANS
QUATERNARY COMPOUNDS
RADIOISOTOPES
RODENTS
SYNTHESIS
VERTEBRATES
400702* - Radiochemistry & Nuclear Chemistry- Properties of Radioactive Materials
550601 - Medicine- Unsealed Radionuclides in Diagnostics