Despite the lower amount of gadolinium in the standard dose of Gd-EOB-DTPA, the results showed that the arterial enhancement in Gd-EOB-DTPA-enhanced dynamic liver MRI was comparable to Gd-DTPA. This result can be explained mainly by the higher relaxivity. Choosing a lower injection rate additionally supported to compensate for the lower injection volume by stretching the bolus without decreasing the peak. In this respect, an injection rate of 1 mL/s showed better results with regard to the arterial enhancement compared with 2 mL/s.

No abstract

The activity of matrix metalloproteinases (MMPs) is elevated locally under many pathological conditions. Gelatinases MMP2 and MMP9 are of particular interest because of their implication in angiogenesis, cancer cell proliferation and metastasis, and atherosclerotic plaque rupture. The aim of this study was to identify and develop a selective gelatinase inhibitor for imaging active MMP2/MMP9 in vivo. We synthesized a series of N-sulfonylamino acid derivatives with low to high nanomolar inhibitory potencies. (R)-2-(4-(4-Fluorobenzamido)phenylsulfonamido)-3-(1H-indol-3-yl)propanoic acid (7) exhibited the best in vitro binding properties: MMP2 IC50 = 1.8 nM, MMP9 IC50 = 7.2 nM. Radiolabeling of 7 with no carrier added (18)F-radioisotope was accomplished starting from iodonium salts as precursors. The radiochemical yield strongly depended on the iodonium counteranion (ClO4(-) > Br(-) > TFA(-) > tosylate). (18)F-7 was obtained in up to 20% radiochemical yield (decay corrected), high radiochemical purity, and >90 GBq/μmol specific radioactivity. The radiolabeled compound showed excellent stability in vitro and in mice in vivo.

Full-dose gadolinium MRA results in higher image quality and significantly higher SNR compared with the half dose. Gadobutrol and Gd-BOPTA have similar enhancement properties at full dose but at half dose, gadobutrol appears superior.