Handbook of Nuclear Chemistry: Radiochemistry and Radiopharmaceutical Chemistry in Life Sciences, Volume 4

Chapter 4: 11C: Labeling Chemistry and Labeled Compounds

G.Antoni, T.Kihlberg, B.L ngstr m

Uppsala Imanet AB, P.O. Box 967, S-751 09 Uppsala, Sweden

SUMMARY:

Methods for the synthesis of compounds labeled with the short-lived positron emitting radionuclide 11C are described. Important aspects on how to achieve high specific radioactivity and the need for technical solution to establish a reproducible routine tracer production are pointed out. Examples of PET as a tool in drug development are also included.

1. INTRODUCTION

The possibility to quantify in vivo biochemistry non-invasively using compounds labeled with radioactive isotopes is a milestone in medical imaging. The first production of the short-lived positron emitting radionuclide 11C was performed in 1934 (Crane and Lauritsen 1934). It was found that 11C decays with a half-life of 20.4 min by positron emission to the stable nuclide 11B. Due to its favorable decay characteristics (98.1% by ? + emission, 0.19% by electron capture) it was recognized as a useful tool in medical imaging. The first biological experiment using 11C was performed by Ruben in 1939 who studied the photosynthesis in plants using [ 11C]carbon dioxide (Ruben et al. 1939). This was followed by Tobias who in 1945 investigated the fixation of [ 11C]carbon monoxide by red blood cells in humans (Tobias et al. 1945). The possibility to prepare more complex molecules and to choose labeling position has significantly contributed to the versatility of the positron emission tomography (PET) technique. In this chapter the most important labeling methods are presented with...

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