Optimization and tissue distribution of [125I]iododomperidone as a radiotracer for D2-receptor imaging

Khater, Safaa I.; El-Sharawy, Dina M.; Refaye, Marwa S. El; Farrag, Nourihan S.

doi:10.1007/s10967-020-07236-z

Cited by 16 publications

(6 citation statements)

References 27 publications

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“…Various body organs such as the heart, liver, kidney, lung, heart, and right and left thigh muscles (normal and infected) were isolated and washed with saline and weighed and counted for their radioactivity content using gamma counter. The blood sample was collected by cardiac-puncture and radioactivity in blood, muscles and bones calculated as 7, 40, and 10% of total animal body-weight, respectively . The data of tissue distribution study were represented as % injected dose/gram organ (% ID/g).…”

Section: Methodsmentioning

confidence: 99%

New Thiophenyl-pyrazolyl-thiazole Hybrids as DHFR Inhibitors: Design, Synthesis, Antimicrobial Evaluation, Molecular Modeling, and Biodistribution Studies

Dawood,

Sayed,

Tohamy

et al. 2023

ACS Omega

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The antibiotic resistance problems constitute a considerable threat to human health worldwide; thus, the discovery of new antimicrobial candidates to conquer this issue is an imperative requirement. From this view, new thiophenyl-pyrazolyl-thiazole hybrids 3–10 were synthesized and screened for their antibacterial efficiency versus Gram – and Gram + bacterial strains compared to the reference drug amoxicillin. It was noticed that the new hybrids displayed significant antibacterial efficacy versus Gram – bacteria, especially against Pseudomonas aeruginosa. Also, all the screened candidates demonstrated a noticeable antifungal effect against Candida albicans (MICs = 3.9–125 μg/mL) relative to fluconazole (MIC = 250 μg/mL). Moreover, the new hybrids were investigated for their antituberculosis potency against Mycobacterium tuberculosis (RCMB 010126). Derivatives 4c, 6b, 8b, 9b, and 10b demonstrated prominent antituberculosis efficiency (MICs = 0.12–1.95 μg/mL) compared with the reference drug isoniazid (MIC = 0.12 μg/mL). The latter derivatives were further assessed for their inhibitory potency versus M. tuberculosis DHFR enzyme. The compounds 4c, 6b and 10b presented a remarkable suppression effect with IC50 values of 4.21, 5.70, and 10.59 μM, respectively, compared to that of trimethoprim (IC50 = 6.23 μM). Furthermore, biodistribution profile using radiolabeling way revealed a perceived uptake of 131I-compound 6b into infection induced models. The docking study for the new hybrids 4c, 6b, 8b, 9b and 10b was performed to illustrate the various binding modes with Mtb DHFR enzyme. In silico ADMET studies for the most potent inhibitors 4c, 6b and 10b were also accomplished to predict their pharmacokinetic and physicochemical features.

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Section: Methodsmentioning

confidence: 99%

New Thiophenyl-pyrazolyl-thiazole Hybrids as DHFR Inhibitors: Design, Synthesis, Antimicrobial Evaluation, Molecular Modeling, and Biodistribution Studies

Dawood,

Sayed,

Tohamy

et al. 2023

ACS Omega

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“…The computer modeling revealed that the labeled complex has an optimal fit (Energy = − 102.05 kcal/mole) to the ligand binding site of the target protein [19,20]. [42]. The brain/blood ratio results indicated that the optimum time for using [ 99m Tc] fonturacetam hydrazide as a radiotracer for brain imaging was 15-60 min.…”

Section: In Silico Assessmentmentioning

confidence: 99%

Radiolabeling and evaluation of fonturacetam hydrazide as a radiotracer for visualization of brain function

El-Kawy

Shweeta

Sallam

2023

J Radioanal Nucl Chem

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Abstract[99mTc] fonturacetam hydrazide was radiosynthesized to assess neuropsychiatric disorders by targeting the brain. The nootropic drug was labeled with technetium-99m, and factors affecting the labeling yield were studied. At optimum conditions, the radiocomplex was obtained at a high radiochemical yield (98.9%) and was stable in saline for up to 36 h and serum for more than 24 h. Labeled fonturacetam hydrazide was characterized and assessed in silico. Biodistribution studies in mice showed that the brain uptake of the complex was 8.8% injected dose per gram (% ID/g) at 5 min post-injection, surpassing the commercially available [99mTc] ECD (4.7% ID/g) and [99mTc] HMPAO (2.25% ID/g). All results suggested that the tracer is a good candidate to image the human brain for assessing neuropsychiatric disorders.

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“…The injected dose was considered to be per gram (ID/gram) . The blood, bone, and muscles were predicted to be 7%, 10%, and 40% from the total body weight, respectively [14][15].…”

Section: -Biological Distribution Of 99m Tc-pip In Normal and Tumored...mentioning

confidence: 99%

Bioevaluation of 99mTc-Pipazethate as a potential guide tracer for malignant tumor imaging.

Refaye

Khater

sharawy

2022

Arab Journal of Nuclear Sciences and Applications

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Diagnosis of tumor is one of the most important stages in the treatment, as good quality imaging and accurate analysis means to choose the right and more effective tracer. Therefore, the study of the ability of new radiopharmaceutical compound to track solid tumor became a pioneering field. Thus, the study of pipazethate as a possible solid tumor marker was in our scope. It was labeled with technetium reaching a (RCY) radiochemical yield of 96.5%, using SnCl2 .2H2O as a reducing agent. A biodistribution study of 99m Tc-Pip in tumored mice was performed which revealed the capability of the complex to image solid tumor as it was accumulated in the tumor with a concentration of 13% at 30min (p.i) post injection T/NT ratio was considered, the ratio reached 2.9 at 30 min postinjection, and this value confirmed the high sensitivity and selectivity of 99m Tc-Pip to tumor. 99m Tc-Pip passed the (BBB) blood brain barrier reaching the brain in a concentration of 5.8g/tissue at 5 p.i in normal mice while it reached 5.5 g/tissue at 5 p.i in tumored mice. Finally, molecular modeling was applied for prediction of the most energetically stable structure of 99m Tc-pip.

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Optimization and tissue distribution of [125I]iododomperidone as a radiotracer for D2-receptor imaging

Cited by 16 publications

References 27 publications

New Thiophenyl-pyrazolyl-thiazole Hybrids as DHFR Inhibitors: Design, Synthesis, Antimicrobial Evaluation, Molecular Modeling, and Biodistribution Studies

New Thiophenyl-pyrazolyl-thiazole Hybrids as DHFR Inhibitors: Design, Synthesis, Antimicrobial Evaluation, Molecular Modeling, and Biodistribution Studies

Radiolabeling and evaluation of fonturacetam hydrazide as a radiotracer for visualization of brain function

Bioevaluation of 99mTc-Pipazethate as a potential guide tracer for malignant tumor imaging.

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