[C]MeAIB uptake occurred principally via a Na-dependent A type mechanism whereas [H]MET uptake occurred predominantly via a Na-independent L type mechanism although other transporters were also utilized depending on cell type. There was no correlation between [H]MET uptake and total system L amino acid transporter (LAT) expression. In contrast, [C]MeAIB uptake strongly correlated with total system A amino acid transporter (SNAT) expression and proliferative activity in this preliminary study using four human carcinoma cell lines. Carcinoma proliferative activity also correlated with total SNAT expression. Advances in Knowledge and Implications for Patient Care: Because there is a significant correlation between the accumulation of [C]MeAIB and the gene expression level of total SNAT as well as the accumulation of [H]FLT, it is suggested that use of the analog [C]MeAIB in PET may provide an indication of tumor cell proliferative activity. [C]MeAIB is therefore expected to be very useful in PET imaging.

In this study, we evaluated the use of 15-(4-¹²³I-iodophenyl)-3(R,S)-methylpentadecanoic acid (¹²³I-BMIPP) to visualize fatty acid metabolism in bacteria for bacterial infection imaging. We found that ¹²³I-BMIPP, which is used for fatty acid metabolism scintigraphy in Japan, accumulated markedly in Escherichia coli EC-14 similar to ¹⁸F-FDG, which has previously been studied for bacterial imaging. To elucidate the underlying mechanism, we evaluated changes in ¹²³I-BMIPP accumulation under low-temperature conditions and in the presence of a CD36 inhibitor. The uptake of ¹²³I-BMIPP by EC-14 was mediated via the CD36-like fatty-acid-transporting membrane protein and accumulated by fatty acid metabolism. In model mice infected with EC-14, the biological distribution and whole-body imaging were assessed using ¹²³I-BMIPP and ¹⁸F-FDG. The ¹²³I-BMIPP biodistribution study showed that, 8 h after infection, the ratio of ¹²³I-BMIPP accumulated in infected muscle to that in control muscle was 1.31 at 60 min after ¹²³I-BMIPP injection. In whole-body imaging 1.5 h after ¹²³I-BMIPP administration and 9.5 h after infection, infected muscle exhibited a 1.33-times higher contrast than non-infected muscle. Thus, ¹²³I-BMIPP shows potential for visualizing fatty acid metabolism of bacteria for imaging bacterial infections.

The effectiveness of L- and D-amino acids for detecting the early stage of infection in bacterial imaging was compared. We evaluated the accumulation of ³H-L-methionine (Met), ³H-D-Met, ³H-L-alanine (Ala), and ³H-D-Ala in E. coli EC-14 and HaCaT cells. Biological distribution was assessed in control and lung-infection-model mice with EC-14 using ³H-L- and D-Met, and ¹⁸F-FDG. A maximum accumulation of ³H-L- and D-Met, and ³H-L- and D-Ala occurred in the growth phase of EC-14 in vitro. The accumulation of ³H-L-Met and L-Ala was greater than that of ³H-D-Met and D-Ala in both EC-14 and HaCaT cells. For all radiotracers, the accumulation was greater in EC-14 than in HaCaT cells at early time points. The accumulation was identified at 5 min after injection in EC-14, whereas the accumulation gradually increased in HaCaT cells over time. There was little difference in biodistribution between ³H-L-and D-Met except in the brain. ³H-L- and D-Met were sensitive for detecting areas of infection after the spread of bacteria throughout the body, whereas ¹⁸F-FDG mainly detected primary infection areas. Therefore, ¹¹C-L- and D-Met, radioisotopes that differ only in terms of ³H labeling, could be superior to ¹⁸F-FDG for detecting bacterial infection in lung-infection-model mice.

Gastrointestinal tract absorption of cationic anticancer drugs and medicines was estimated using whole-body imaging following oral [¹²³I]MIBG administration. [¹²³I]MIBG was added to cultures of human embryonic kidney (HEK)293 cells expressing human organic anion transporting polypeptide (OATP)2B1, carnitine/organic cation transporter (OCTN)1 and OCTN2, and organic cation transporter (OCT)1, OCT2, and OCT3 with and without cimetidine (an OCTN and OCT inhibitor) and L-carnitine (an OCTN inhibitor). Biodistribution analyses and single-photon emission computed tomography (SPECT) imaging in normal and dextran sodium sulfate (DSS)-induced experimental colitis mice were conducted using [¹²³I]MIBG with and without cimetidine. [¹²³I]MIBG uptake was significantly higher in HEK293/OCTN1, 2, and OCT1-3 cells than in mock cells. Uptake via OCTN was inhibited by L-carnitine, whereas OCT-mediated uptake was inhibited by cimetidine. Biodistribution analyses and SPECT imaging studies showed significantly lower accumulation of [¹²³I]MIBG in the blood, heart, liver, and bladder in DSS-induced experimental colitis mice and mice with cimetidine loading compared with normal mice, whereas significantly higher accumulation in the stomach and kidney was observed after [¹²³I]MIBG injection. [¹²³I]MIBG imaging after oral administration can be used to estimate gastrointestinal absorption in the small intestine via OCTN and/or OCT by measuring radioactivity in the heart, liver, and bladder.

Background The aims of this study were (1) to evaluate the impact of injection dose, post-reconstruction filtering, and collimator choice on image quality of myocardial perfusion single-photon emission computed tomography (SPECT) using cadmium-zinc telluride (CZT) detectors and (2) to determine how these factors affect measured infarct size in the in vivo rat. Methods Twenty-four healthy and eight myocardial infarct (MI) rats underwent myocardial perfusion SPECT imaging after injection of various doses (25 to 200 MBq) of 99mTc-tetrofosmin using a standard (STD) five-pinhole collimator and high-sensitivity (HS) five-pinhole collimator. Image quality score, contrast-to-noise ratio, sharpness index, coefficient of variation (CV), and measured defect size were assessed as measures of image quality. Results The image quality score increased and CV decreased as a function of injection dose. The contrast-to-noise ratio increased and sharpness index decreased as a function of Gaussian kernel size. When STD and HS were compared, HS tended to show higher image quality score and lower CV than STD. The use of post-reconstruction filter significantly improved image quality score and lessened CV. The reproducibility of defect size measurements, as assessed by intraclass correlation coefficients (ICC), between the collimators was poor-to-moderate (ICC = −0.31~0.57) with low (25 MBq) injection dose and with no or light (1.5-mm kernel size) filtering, whereas it was good-to-excellent (ICC = 0.75~0.97) with high (200 MBq) dose or low dose with heavy (2.5-mm kernel size) filtering. The filtering-related reproducibility was poor (ICC = −0.18~0.17) for STD with low injection dose, whereas it was good-to-excellent (ICC = 0.79~0.89) for HS. Furthermore, there was a filtering-related underestimation of defect size particularly with the use of heavy smoothing. Conclusions Appropriate imaging setting is important to obtain high quality images and thereby reliable measurements using a preclinical myocardial SPECT in the rat. When only a low injection dose (25 MBq) is allowed, we would recommend to use HS with light (1.5-mm kernel size) filtering.