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15-(p-[⁷⁵Br]bromophenyl)pentadecanoic Acid: Pharmacokinetics and Potential as Heart Agent

Institut für Chemie 1(Nuklearchemie) der Kernforschungsanlage Jülich GmbH, Jülich, Germany

Correspondence: For reprints contact: Prof. Dr. G. Stöklin, Institut für Chemie 1 (Nuklearchemie), Kernforschungsanlage Jülich GmbH, Postfach 1913, D-5170 Jülich, FRG.

ABSTRACT

Preparation, quality control, and pharmacokinetics of 15-(p-[⁷⁵Br]bromophenyl)-pentadecanoic acid (BPPA) were studied, with particular emphasis on the fate of the label and the usefulness of BPPA as a heart agent. BPPA labeled with the positron emitter Br-75 (T_1/2 = 98 min) was prepared in 55% radiochemical yield with a specific activity of 1000 Cl/mmol. While the uptake of BPPA in the heart muscle is as fast and efficient as that of aliphatic -halofatty acids, its elimination is delayed, owing mainly to an inhibited ß oxidation and the formation of lipophilic catabolites. The blood activity and its time course are identical to those of -halofatty acids, but no free bromide appears in any body fluid or organ. The complex pharmacokinetic behavior of stable lipophilic catabolites prevents a quantitative background correction. In contrast to aliphatic -halofatty acids, a quantitative evaluation of myocardial metabolism is not possible. Br-75 BPPA, however, is well suited for positron emission tomography of the heart.