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In this work, the complex of [99mTc]tricarbonyl pantoprazole was labeled utilizing a [99mTc]tricarbonyl core. Many optimum parameters have been used such as substrate (200 μg), pH of the reaction mixture (9.5), reaction time (30 minutes), as well as temperature (100°C), providing an optimal radiochemical purity of 96.0%. Biodistribution investigations of our radiotracer, [99mTc]tricarbonyl pantoprazole, were conducted on 3 sets of mouse models: a normal mice group, Helicobacter pylori pretreated mice as a microbial model group, and a chemical model (chemically induced stomach ulcer). The results indicated maximum stomach uptakes in three models of 12.5, 29.6, and 37.9 %ID/gram tissue at 60 min post injection (p.i.) respectively. [99mTc]Tricarbonyl pantoprazole complex may be an excessively bio-selective receptor-tracer for peptic ulcer imaging, particularly for the microbial model group. [ABSTRACT FROM AUTHOR]

A procedure was developed for preparing [99mTc]-tricarbonyl-5-[(3-carboxy-4-hydroxyphenyl)diazenyl]-2-hydroxybenzoic acid complex ([99mTc]-tricarbonyl-Olsalazine), for ulcerative colitis (UC) imaging. High yield and 98.5% radiochemical purity of [99mTc]-tricarbonyl-Olsalazine were reached under optimized conditions. Thin layer chromatography (TLC) was used for the purification of the labeled compound. Reversed-phase high-performance liquid chromatography (RP-HPLC) was also used. A biodistribution study performed with a microbial mouse model of UC showed that the colon localization of [99mTc]-tricarbonyl-Olsalazine was the highest (77 ± 1.7% ID/g) at 120 min post injection. The agent was still present in the ulcerated colon for up to 24 h post injection (75% ID/g). Such level was not reached in previous studies. Thus, [99mTc]-tricarbonyl-Olsalazine can be used as a radiotracer for UC imaging in mice. [ABSTRACT FROM AUTHOR]

Cardiac imaging is one of the most important tools for diagnosing many diseases related to the heart. This work was devoted to developing this method using experiments on mice. The formation of a complex of [99mTc]dithiocarbamate of procainamide under optimum conditions of reaction temperature (37°C), reaction time (30 min), pH of the reaction mixture (8), amount of substrate (100 μg), amount of reducing agent tin(II) (content, 50 μg), and stability in rat serum (8 h) was achieved using radioactive Tc-99m (300 – 500 MBq) to give high labeling yield (98.5%) and radiochemical purity. Procainamide works through sodium channel blocker. Normal mice were used in biodistribution investigations. High absorption uptake of the [99mTc]dithiocarbamate of procainamide complex was found to be 33.47 ± 0.83% injected dose/g organ (ID/g) as observed in mice for up to 5 min, which demonstrated its usefulness as a radiotracer for heart imaging. [ABSTRACT FROM AUTHOR]

This work centralizes on pursuit ulcerative colitis localized in mice. High radiolabeling and purity were ensured during the formation of a radiotracer, [99mTc]nitrido-mesalamine complex, due to inspecting many parameters under optimum conditions including pH of the reaction mixture (pH 6), reducing agent content (tin(II), 50 μg), reaction time (30 min), mesalamine content (200 μg), Tc-99m (200 – 350 MBq), stability in rat serum (24 h), and reaction temperature (37°C) giving high radiolabeling yield of 98%. In silico molecular docking study was performed to evaluate the possible mechanism of action on the target peroxisome proliferator-activated receptor gamma (PPARγ). Results of biological studies obtained in this work illuminate the usefulness of [99mTc]nitrido-mesalamine complex as a radiotracer that can be used for ulcerative colitis imaging up to 24 h in microbial model (76% dose/g organ (ID/g)) as monitored in mice. [ABSTRACT FROM AUTHOR]

The radiotracer [99mTc]tricarbonyl Rabeprazole was successfully prepared using the [99mTc]tricarbonyl precursor. The reaction conditions were optimized (200 µg/2 mL substrate concentration, pH 8, incubation temperature 100°C, 30 min) to achieve the maximum radiochemical purity of 98%. Thin layer chromatography (TLC) and high-performance liquid chromatography (HPLC) were used to assess the radiochemical purity and quality control parameters. A biodistribution study was also conducted to evaluate the biological biodistribution of [99mTc]tricarbonyl Rabeprazole in three different groups of mice models, with the normal group serving as the control and the second and third groups being microbial and chemically induced stomach ulcer disease models, respectively. The radiotracer [99mTc]tricarbonyl Rabeprazole complex was administered intravenously into mice via the tail vein and dissected at predefined time intervals. The biodistribution data demonstrated that the maximum absorption of [99mTc]tricarbonyl Rabeprazole complex in the stomach of normal mice and microbially and chemically induced ulcerated mice were 9.5, 35.3, and 23.7% ID/g tissue at 1 h post injection, respectively. The outcomes of the research show that [99mTc]tricarbonyl Rabeprazole can be used as a promising imaging agent to diagnose stomach ulcers. [ABSTRACT FROM AUTHOR]

[99mTc]Tricarbonyl Omeprazole was prepared using [99mTc]tricarbonyl core. The radiochemical conversion of 98.0% was reached under optimized reaction conditions: substrate amount 100 µg, pH 8, reaction time 30 min, 100°C. Three different groups of mice models were used in biodistribution studies of [99mTc]tricarbonyl Omeprazole: normal group, microbial model group (using Helicobacter pylori), and induced ulcerated mice (chemical model). The stomach uptake in three models was 10.5, 38.7, and 29.6% ID/g at 1 h post injection. This, [99mTc]tricarbonyl Omeprazole can be considered as a highly selective radiotracer for peptic ulcer imaging, especially in microbial model group. [ABSTRACT FROM AUTHOR]

This work focuses on tracking peptic ulcer localized in mice. The formation of a [99mTc]dithiocarbamate of famotidine complex at optimum conditions of reaction temperature (37 °C), reaction time (30 min), pH of the reaction mixture (5), amount of substrate (100 µg), amount of reducing agent (tin (II) content, 50 µg), was achieved using radioactive Tc-99m (250–400 MBq), with labelling yield of 98% and high radiochemical purity. The in-vitro stability of [99mTc]dithiocarbamate of famotidine complex was shown to be high in rat serum for up to 8 h. Normal and ulcerated mice were used in biodistribution studies. Famotidine works by blocking histamine-2-receptor antagonists (H2RAs). The high absorption of [99mTc]dithiocarbamate of famotidine complex in stomach in amount of 27.15% injected dose/g organ (ID/g) observed in ulcerated mice for up to 24 h demonstrated its usefulness as a novel radiotracer for stomach imaging. [ABSTRACT FROM AUTHOR]

A complex of 99mTc tricarbonyl with Mesalamine for ulcerative colitis imaging was prepared and studied. Several factors such as substrate concentration, pH, reaction period, and reaction temperature were optimized to achieve the highest radiochemical yield and purity. Under optimum conditions, the radiochemical yield of synthesized 99mTc tricarbonyl Mesalamine radiotracer reached 98%. The labeled compound was separated and purified using thin-layer chromatography (TLC) and reversed-phase high-performance liquid chromatography (RP-HPLC). According to biodistribution investigations in a microbial mouse model of ulcerative colitis, the colon localization of 99mTc tricarbonyl Mesalamine was the highest (77.4 ± 1.7%) in 120 min after injection. Thus, 99mTc tricarbonyl Mesalamine can be used as a radiotracer for imaging ulcerative colitis. [ABSTRACT FROM AUTHOR]

About 35% reduction in cancer deaths among patients having solid tumors is related to using aspirin, which encouraged us to develop a new specific tumor diagnostic radiopharmaceutical agent. This can be done by direct labeling of aspirin with technetium-99m using stannous chloride as a reductant at pH 9. At this pH, aspirin is saponificated to salicylate ions. Salicylate binds to pertechenetate to form 99mTc salicylate complex. The radiochemical yield (RCY, %) of 99mTc-salicylate complex obtained from aspirin was determined using paper chromatography, electrophoresis, and HPLC and was found to reach 90.2%. The 99mTc salicylate complex obtained from aspirin was stable for up to 5 h. The tumor uptake of the 99mTc salicylate complex obtained from aspirin was determined by ex-vivo study in tumor-bearing mice. This study showed that 99mTc salicylate complex was concentrated in tumor sites (ascites or solid), allowing tumor radioimaging. High target/non-target (tumor muscles/normal muscles) uptake ratio shows that 99mTc salicylate complex can be utilized for early detection of solid tumors. Molecular modeling and docking study conofirm the possibility of using the radiolabeled 99mTc salicylate complex for specific cancer imaging in binding with epidermal growth factor receptors (EGFR). [ABSTRACT FROM AUTHOR]

Two 99mTc cores, 99mTc tricarbonyl and 99mTc-Sn(II), are compared in labeling of Lansoprazole (Lans). The optimum conditions of Lansoprazole labeling with 99mTc in the presence of SnCl2·2H2O as a reducing agent are as follows: pH 8, 100 μg of SnCl2·2H2O, room temperature, 2 mg of lansoprazole, and 30 min; the maximum radiochemical yield was 98 ± 0.22%. The obtained 99mTc Lansoprazole complex was stable in serum for up to 16 h. The optimum conditions of Lansoprazole binding with the 99mTc tricarbonyl ([99mTc(CO)3(H2O)3]+) core are as follows: pH 8, 2 mg of Lansoprazole, 100°С, 30 min. The complex was stable in serum for up to 12 h. Biodistribution study of the first core on two different groups of mice (control group and ulcer-bearing group) showed comparatively high uptake in the ulcer group of mice, 77.8 ± 1.1% ID/g at 30 min post-injection (higher than for the control group); at 24 h, the uptake decreased to 17.9% ID/g. Similar results were obtained with 99mTc tricarbonyl Lansoprazole: 78.5% ID/g at 30 min post-injection and 24.6% at 24 h. Thus, both complexes are suitable as radiotracers for stomach ulcer imaging. [ABSTRACT FROM AUTHOR]

99mTc nitrido-Levetiracetam was prepared using the 99mTc nitrido core for labeling. The reaction conditions were optimized to get the highest radiochemical purity (98%): substrate amount 2 mg, Sn(II) (reducing agent) amount 50 µg, pH 7, 30 min, ambient temperature. The biodistribution studies revealed high brain uptake of 99mTc nitride-Levetiracetam, reaching a maximum of 9% ID/g at 30 min post injection (p.i.). The complex deserves further analysis as a candidate brain imaging agent. [ABSTRACT FROM AUTHOR]

Irbesartan was labeled using 125I or 131I with N-bromosuccinimide (NBS) as an oxidizing agent. A lot of operators such as, quantity of substrate, the quantity of oxidizing agent, reaction temperature, reaction time, and pH of reaction medium were studied to optimize high radiochemical yield of [125I]IodoIrbesartan ([125I]Irb.). The preclinical evaluation of IodoIrbesartan in experimental mice indicated high accumulation in target organ of heart with a high heart/blood ratio of 12.85 at 30 min post-injection. This study indicates the suitability of [125I]IodoIrbesartan ([125I]Irb.) for cardiac imaging. [ABSTRACT FROM AUTHOR]

Azathioprine, an antitumor agent, was labeled with 99mTc using stannous chloride dihydrate as a reducing agent. Factors such as the amounts of the reducing agent and substrate, pH, and reaction temperature and time were systematically studied to determine the optimum conditions, under which the 95% radiochemical yield was achieved. Biodistribution studies demonstrate the suitability of 99mTc-azathioprine as a novel tracer for tumor imaging. It shows high selectivity to high-replicating solid tumors. [ABSTRACT FROM AUTHOR]

Labetalol was labeled with 188Re. The reaction conditions (amounts of stannous chloride and substrate, pH, time) were optimized, and the radiochemical yield as high as 95 ± 0.4% was reached. Biodistribution in mice was studied. 188Re-Labetalol showed excellent initial heart uptake and good retention. The heart/liver ratios were 5.16, 2.70, and 2.15 at 30, 60, and 120 min post injection, respectively. [ABSTRACT FROM AUTHOR]

Tc-tricarbonyl-labeled chenodiol (chenodeoxycholic acid, CDCA) intended for hepatobiliary imaging was prepared by 30-min heating at 100°C with a radiochemical yield of >98%. The radiolabeling yield and stability of the complex were evaluated using different chromatographic techniques. Biodistribution studies in Albino Swiss mice at different time intervals after administration of the complexes showed that the maximum uptake of the complexes in the liver was 35.5 ± 0.25% ID/g at 30 min post injection. Tc-tricarbonyl- CDCA shows promise for hepatobiliary imaging. [ABSTRACT FROM AUTHOR]

Famotidine was labeled with iodine-125 to obtain 125I-famotidine (125I-fam) as an agent for ulcer imaging. The radiochemical yield of 125I-famotidine reached approximately 98.5 ± 0.23% at optimum conditions of pH, oxi- dizing agent, reaction time and the amount of substrate. 125I-fam was stable for 48 h. Different chromatographic techniques were used to determine the radiochemical yield and purity. Intravenous biodistribution studies of 125I-fam revealed high concentration in the stomach ulcer, reaching about 65.9 ± 0.28% of the total injected dose at 30 min post injection. This concentration of 125I-fam in stomach ulcer makes this agent promising for stomach ulcer imaging. [ABSTRACT FROM AUTHOR]

Lung imaging radiopharmaceuticals are helpful agents for measuring pulmonary blood flow and allow detection of pulmonary embolism and lung cancer. The goal of this study was to develop a novel potential radiopharmaceutical for lung imaging. Zolmitriptan (a selective serotonin receptor agonist) was successfully labeled with Tc via direct labeling method under reductive conditions studying different factors affecting the labeling efficiency. Tc-zolmitriptan was obtained with a maximum labeling yield of 92.5 ± 0.61 % and in vitro stability up to 24 h. Molecular modeling was done to predict the structure of Tc-zolmitriptan and ensure that radiolabeling did not affect binding ability of zolmitriptan to its receptor. Biodistribution studies showed that maximum lung uptake of Tc-zolmitriptan was 23.89 ± 1.2 % injected dose/g tissue at 15 min post-injection and retention in lungs remained high up to 1 h, whereas the clearance from mice appeared to proceed mainly via the renal pathway. Scintigraphic images confirmed the biodistribution results showing a high resolution lung image with low accumulation of radioactivity in other organs except kidneys and urinary bladder. Tc-zolmitriptan is not a blood product and so it is more safe than the currently available Tc-MAA, and its lung uptake is higher than that of the recently discovered I-IPMPD, Tc(CO)I and Tc-DHPM. So, Tc-zolmitriptan could be used as a hopeful radiopharmaceutical for lung scintigraphic imaging. [ABSTRACT FROM AUTHOR]

Mesalamine was labelled with technetium-99m (Tc) in high radiolabelling yield (~98.4 %), in vitro stability (~4 h) and in serum persistence (~24 h). Optimum labelling conditions were investigated. The structure of the complex was confirmed using in silico analysis. Molecular docking was performed to evaluate the complex binding to its biochemical target, the PPARγ receptor. Biodistribution and clearance studies were performed in normal and ulcerative colitis models in mice. The tracer's localization was highest (~65.2 %) in microbial model compared to chemical model (~42.4 %) and normal mice (~22.1 %) at 60 min post injection. All data supported the usefulness of Tc-mesalamine as a radiotracer for ulcerative colitis. [ABSTRACT FROM AUTHOR]

Purpose: Zearalenone (ZEN) which is one of the known fusarium species mycotoxin, produced primarily on many cereal crops. Consequently, the current study aims to estimate the possibility of labeling zearalenone and the pattern of accumulation of the produced labeled zearalenone [ 125 I]-ZEN in different mice tissues, and the possible protective effect of Lactobacillus plantarum to reduce organ accumulation of Zearalenone., Materials and Methods: the experiment was conducted on two groups of mice were used; the two groups received [ 125 I] Zearalenone administered by tail vein injection, the first group receive nothing else while the second group received also L. plantarum (as a control agent) orally. The mice were kept under observation for 120 min to monitor zearalenone distribution., Results: by monitoring the zearalenone distribution the maximum concentration was found to be mainly primarily in the intestine (45.8 %) followed by the liver (27.15 %) while in the ovary (the most susceptible organ was (3.22 %) after120 min, in the first group of mice. The same pattern was observed in the second group with concentrations of (46.1 %), (30.19 %) and (0.09 %) in the intestine, liver respectively., Conclusion: These results indicated the lactic acid bacteria played a role in decreasing labeled zearalenone in the ovaries which is the target organ. [ 125 I]-labeled ZEN is a promising novel tracer for organ imaging and that a significant role that L. plantarum could play in decreasing the zearalenone bioavailability of in mice organs., Competing Interests: The authors report no declarations of interest., (© 2022 The Author(s).)

Nizatidine has been labeled using [ 125 I] with chloramine-T as oxidizing agent. Factors such as the amount of oxidizing agent, amount of substrate, pH, reaction temperature, and reaction time have been systematically studied to optimize the iodination. Biodistribution studies indicate the suitability of radioiodinated nizatidine as a novel tracer to image stomach ulcer. Radioiodinated nizatidine may be considered a highly selective radiotracer for peptic ulcer imaging., (Copyright © 2017 John Wiley & Sons, Ltd.)

The goal of the study aims to evaluate newly radioiodinated candesartan (CAN) as a potential cardiovascular tracer. CAN was labeled using 125 I with chloramine-T (Ch-T) and N-bromosuccinimide (NBS) with full characterization of cold Iodo-candesartan. Factors such as pH, reaction temperature, reaction time, substrate, and oxidizing agent amounts were studied to optimize the radioiodination of CAN. The optimum radiochemical yield of 125 I-CAN was 98%. The labeled compound was separated and purified using high-pressure liquid chromatography. The biological distribution indicates the suitability of 125 I-CAN as a novel tracer to detect cardiovascular disorders., (Copyright © 2016 John Wiley & Sons, Ltd.)