Myocardial extraction and subcellular distribution of new types of technetium-labeled fatty acids


Myocardial extraction and subcellular distribution of new types of technetium-labeled fatty acids

Mirtschink, P.; Stehr, S. N.; Heintz, A.; Pexa, A.; Wunderlich, G.; Walther, M.; Pietzsch, H.-J.; Spies, H.; Jung, C.; Kraus, W.; Kropp, J.; Deussen, A.

SPECT- images performed with radiolabeled fatty acids (FA) allow detailed studies about the heart function, because flow and metabolism are represented. Up to now, only 123iodinated FA are available for myocardial viability diagnostics in some parts of the world, but the application is limited due to serious disadvantages: first, the expensive production of pure 123I requires a cyclotron and second, the radiolabeled FA compounds must be purchased by outside vendors which resulted in disproportional costs and logistical problems. 99mTc, has ideal physical properties for SPECT-imaging (Eγ-= 140 keV), a short half- life of 6 h, and is available through a 99Mo/99mTc generator whenever needed. The development of 99mTc- labeled FA has been a goal of various research groups in the past. Despite many different approaches, no appropriate 99mTc compound with similar myocardial extraction properties as found with BMIPP and DMIPP is available to date. Most previous work in this field has focused on radiometal coordination by use of a polar tetradentate N2S2 chelate with a central oxometal(V) core. We concentrated on the development and experimental evaluation of alternative coordination moieties according to the ‘4+1’ mixed ligand approach to create newly technetium labeled FA with an improved myocardial profile. In the ‘4+1’ donor atom arrangement, 99mTc is coordinated by both a tetradentae ligand and by a monodentate bearing the FA moiety. This system is rather lipophilic and show high stability towards, e.g. challenging SH-agents. While the conventional ‘4+1’ 99mTc FA are built on in the sequence Tc-chelate, alkyl chain (a), carboxyl group (c) ->(Tc-a-c) we also developed and investigated some compounds with a new design according to the sequence carboxyl group (c), alkyl chain, Tc chelate, lipophilic tail (lt) -> (c – a – Tc – lt), transferring the 99mTc chelate from the end- to a more central position of the compound.

  • Lecture (Conference)
    ESRR'06 - European Symposium on Radiopharmacy and Radiopharmaceuticals, 30.03.-02.04.2006, Lucca, Italy
  • Abstract in refereed journal
    Quarterly Journal of Nuclear Medicine and Molecular Imaging 50(2006)Suppl 1, 20-21

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Publ.-Id: 8497