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Labelling methods in (PET-)Radiopharmacy: Do we need alternatives?Steinbach, J.
Labelling of molecules was introduced by Georg von Hevesy already decades ago utilizing radiophosphorus. With the availability of C-14 and H-3 a long period of isotopic labelling started in the fifties of the last century following Rudolf Schönheimer´s idea to label biomolecules with deuterium. This was the scientific base of the modern biochemistry enabling detailed study of metabolism and of modern pharmacokinetics. With the use of radioiodine fur human investigations and therapy the era of Nuclear Medicine began during that time.
All these applications require different labelling techniques for the radiotracer synthesis. Most of them have been derived from organic microchemistry and have been further developed for the special radiochemical conditions such as radiation protection and the limited amount of substance matter.
The introduction of radiometals to Nuclear Medicine, first of all Tc-99m, opened a new challenge. This was the need to mimic organic molecules by coordination compounds utilizing knowledge from inorganic, organic and radiochemistry.
At the end of the seventies the Positron Emission Tomography came into the focus of science and later on of medicine. Completely new methods had to be developed due to the application of the no carrier added positron emitting radionuclides in connection with their short half lifes first of all for F-18 and C-11.
Nowadays thousands of compounds have been labelled organic and inorganic. Hundreds of methods have been developed to introduce e.g. carbon isotopes, radiohalogens and radiometals into the desired positions of molecules comprising a wide variety of substance classes.
Have we reached a saturation of demand for labelling methods?
Of course for small molecules the requirements for real new developments may be limited. But new demands are at the horizon: This are biomacromolecules such as proteins, peptides, oligonucleotides which are sensitive to the classic conditions of chemical reactions. Other problems are connected with the need for regioselective, site specific labelling.
There is and will be done a lot of work also in the future for applied purposes.
Invited lecture (Conferences)
15th Workshop "The Synthesis and Applications of Isotopes and Isotopically Labelled Compounds", 12.-13.06.2008, Bad Soden, Deutschland
Abstract in refereed journal
Journal of Labelled Compounds and Radiopharmaceuticals 52(2009)7, 257