The Radiopharmaceutical Chemistry of Gallium(III) and Indium(III) for SPECT Imaging

Dilworth, Jonathan R.; Pascu, Sofia I.

doi:10.1002/9781118854754.ch7

Cited by 5 publications

(2 citation statements)

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“…Numerous In(III) and Ga(III) complexes are applied as pharmaceutical agents in connection with their diagnostic and therapeutic properties. Indium-based agents containing 113m In(III) or 111 In(III) have been used in diagnostic nuclear medicine for decades [1][2][3]. A number of In(III)-chelates have been tested for the selective delivery of 111 In(III) to various tissues, the tris-ligand complex of 8-hydroxyquinoline (HQ) is the only indium containing product currently approved by the FDA for the detection and diagnosis of infections and inflammatory lesions [2,4].…”

Section: Introductionmentioning

confidence: 99%

“…Indium-based agents containing 113m In(III) or 111 In(III) have been used in diagnostic nuclear medicine for decades [1][2][3]. A number of In(III)-chelates have been tested for the selective delivery of 111 In(III) to various tissues, the tris-ligand complex of 8-hydroxyquinoline (HQ) is the only indium containing product currently approved by the FDA for the detection and diagnosis of infections and inflammatory lesions [2,4]. This HQ complex is not directly injected in the blood, extensive serum protein binding of In(III) necessitates standardized procedures where cellular elements of the blood (principally leukocytes) are separated and labelled with the complex outside the patient's body and then returned to the circulatory system [2,5].…”

Section: Introductionmentioning

confidence: 99%

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Solution speciation and human serum protein binding of indium(III) complexes of 8-hydroxyquinoline, deferiprone and maltol

2022

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Solution speciation and serum protein binding of selected In(III) complexes bearing O,O and O,N donor sets were studied to provide comparative data for In(III) and analogous Ga(III) complexes. Aqueous stability of the In(III) complexes of maltol, deferiprone, 8-hydroxyquinoline (HQ) and 8-hydroxyquinoline-5-sulfonate (HQS) was characterized by a combined pH-potentiometric and UV–visible spectrophotometric approach. Formation of mono, bis and tris-ligand complexes was observed. The tris-ligand complexes of HQ (InQ3) and deferiprone (InD3) are present in solution in ca. 90% at 10 µM concentration at pH = 7.4, while the tris-maltolato complex (InM3) displays insufficient stability under these conditions. Binding towards human serum albumin (HSA) and (apo)transferrin ((apo)Tf) of InQ3, InD3 and InM3 complexes and Ga(III) analogue of InQ3 (GaQ3) together with InCl3 was investigated by a panel of methods: steady-state and time-resolved spectrofluorometry, UV–visible spectrophotometry and membrane ultrafiltration. Moderate binding of InQ3 to HSA was found (log K′ = 5.0–5.1). InD3 binds to HSA to a much lower extent in comparison to InQ3. ApoTf is able to displace HQ, deferiprone and maltol effectively from their In(III) complexes. Protein binding of non-dissociated InQ3 was also observed at high complex-to-apoTf ratios. Studies conducted with the InQ3/GaQ3 – HSA – Tf ternary systems revealed the more pronounced Tf binding of In(III) via ligand release, while the original GaQ3 scaffold is preferably retained upon protein interactions and significant albumin binding occurs. Significant dissociation of InQ3 was detected in human blood serum as well. Graphical abstract

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Solution speciation and human serum protein binding of indium(III) complexes of 8-hydroxyquinoline, deferiprone and maltol

2022

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Overview of Medical and Biological Applications of Indium(III) Complexes

Ajiboye,

Amao,

Adeyemi

et al. 2024

Chemistry Africa

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Indium(III) complexes are versatile species that emit Auger electrons which made them a choice for a wide range of biological and medical applications. The properties of these complexes depend on the primary ligand that was used for their syntheses. Herein, methods of synthesizing xanthates, dithiocarbamate, phthalocyanine, thiosemicarbazone and naphthalocyanine complexes of indium(III) are discussed. Also, the methods for synthesizing indium(III) complexes having other ligands are highlighted. Furthermore, antibacterial, antifungal and antiviral potential of the indium(III) complexes are comprehensively discussed. Other biological applications of the complexes such as anticancer, bioimaging, radiopharmaceutical, photodynamic chemotherapy, antioxidants, and optical limiting applications of these indium(III) complexes are comprehensively reviewed. In addition, toxicity of indium(III) complexes towards biological samples are examined because these must be considered in evaluating the safety and efficacy of indium(III) complexes for these numerous applications. Overall, indium(III) complexes are reported to have displayed a good performance in all these biological and medical applications. The future perspectives on the applications of indium(III) complexes are therefore suggested.

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Indium(III) complexes with 2-acetylpyridine-derived thiosemicarbazones exhibit cytotoxic activity against human leukemia and solid tumor cell lines

et al. 2017

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The Radiopharmaceutical Chemistry of Gallium(III) and Indium(III) for SPECT Imaging

Cited by 5 publications

References 74 publications

Solution speciation and human serum protein binding of indium(III) complexes of 8-hydroxyquinoline, deferiprone and maltol

Solution speciation and human serum protein binding of indium(III) complexes of 8-hydroxyquinoline, deferiprone and maltol

Overview of Medical and Biological Applications of Indium(III) Complexes

Indium(III) complexes with 2-acetylpyridine-derived thiosemicarbazones exhibit cytotoxic activity against human leukemia and solid tumor cell lines

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