Synthesis and Cardiac Imaging of (18)F-Ligands Selective for beta(1)-Adrenoreceptors

[摘要]：A series of potent and selective beta(1)-adrenoreceptor ligands were identified (IC(50) range, 0.04-0.25 nM; beta(1)/beta(2) selectivity range, 65-450-fold), labeled with the PET radioisotope fluorine-18 and evaluated in normal Sprague-Dawley rats. Tissue distribution studies demonstrated uptake of each radiotracers from the blood pool into the myocardium (0.48-0.62% ID/g), lung (0.63-0.97% ID/g), and liver (1.03-1.14% ID/g). Dynamic mu PET imaging confirmed the in vivo dissection studies.

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