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Synthesis of a fluorinated fatty acid, dl-erythro-9,10-[ 18F]difluoropalmitic acid, and biodistribution studies in rats
Ist Teil von
International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology, 1990, Vol.17 (8), p.805-809
Ort / Verlag
England: Elsevier Ltd
Erscheinungsjahr
1990
Quelle
Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)
Beschreibungen/Notizen
9,10-Difluoropalmitic acid (DFPA) labeled with the cyclotron produced, positron emitting radionuclide
18F has been synthesized as a potential analogue of 9,10-[
3H]palmitic acid, a fatty acid which has been used to study lipid metabolism in rat brain and pituitary. [
18F]DFPA was prepared by the direct and stereoselective addition of [
18F]F
2 to the double bond of
cis-9,10-palmitoleic acid. The fluorination was carried out in FCCl
3 at −70 °C using a low concentration of F
2 (0.5%) in neon. [
18F]DFPA has been obtained in radiochemical yields of 12–16% from end-of-bombardment (EOB) in approx. 2.5 h. Chemical and radiochemical purity exceeded 95%, and specific activities calculated to EOB ranged from 500 to 1000 mCi/mmol. [
18F]DFPA crosses the blood-brain barrier and is incorporated into rat brain at about twice the level of that of 9,10-[
3H]palmitic acid. The synthesis of [
18F]DFPA permits us to study the biological disposition and metabolism of a vicinal-difluoro fatty acid.