Potential radiopharmaceuticals for the diagnosis of biliary atresia and neonatal hepatitis: EHPG and HBED chelates of 67Ga and 111In

Hunt, F.C.

doi:10.1016/0883-2897(88)90058-x

Cited by 4 publications

(3 citation statements)

References 9 publications

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“…Although considered a borderline-hard metal, among the metal ions currently discussed, In 3+ is relatively soft ( I A = 6.3). Indium(III) is a versatile metal that can form stable complexes with soft donating groups, such as thiols, ,,, as well as hard donating groups, such as phenolates. ,− Although not as convenient as in the case of the lanthanides, the p K a of aquated In 3+ (p K a = 4.0, In 3+ (aq) → InOH 2+ (aq) ) is generally nonproblematic for radiolabeling.…”

Section: Indiummentioning

confidence: 99%

Radioactive Main Group and Rare Earth Metals for Imaging and Therapy

2018

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Radiometals possess an exceptional breadth of decay properties and have been applied to medicine with great success for several decades. The majority of current clinical use involves diagnostic procedures, which use either positron-emission tomography (PET) or single-photon imaging to detect anatomic abnormalities that are difficult to visualize using conventional imaging techniques (e.g., MRI and X-ray). The potential of therapeutic radiometals has more recently been realized and relies on ionizing radiation to induce irreversible DNA damage, resulting in cell death. In both cases, radiopharmaceutical development has been largely geared toward the field of oncology; thus, selective tumor targeting is often essential for efficacious drug use. To this end, the rational design of fourcomponent radiopharmaceuticals has become popularized. This Review introduces fundamental concepts of drug design and applications, with particular emphasis on bifunctional chelators (BFCs), which ensure secure consolidation of the radiometal and targeting vector and are integral for optimal drug performance. Also presented are detailed accounts of production, chelation chemistry, and biological use of selected main group and rare earth radiometals.

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Section: Indiummentioning

confidence: 99%

Radioactive Main Group and Rare Earth Metals for Imaging and Therapy

2018

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“…In terms of the coordination chemistry of In 3+ , owing to its relatively large ionic size of 62–92 pm, it usually attains a coordination number of 7–8 in its complexes . Although hydrated In 3+ has a high p K a of 4.0, it is usually considered as a borderline acidic metal ion ( I A = 6.3) with affinity for soft donor groups, such as thiols, , as well as hard donor groups, such as phenolates and carboxylates. , While the lanthanide Lu 3+ is a larger metal ion with an ionic radius of 86–103 pm and coordination number 6–9, the metal ion has a strong preference for hard basic donor atoms ( I A = 10.07) such as carboxylates …”

Section: Introductionmentioning

confidence: 99%

“…13 Although hydrated In 3+ has a high pK a of 4.0, 14 it is usually considered as a borderline acidic metal ion (I A = 6.3) with affinity for soft donor groups, such as thiols, 15,16 as well as hard donor groups, such as phenolates and carboxylates. 17,18 While the lanthanide Lu 3+ is a larger metal ion with an ionic radius of 86−103 pm and coordination number 6−9, 13 the metal ion has a strong preference for hard basic donor atoms (I A = 10.07) such as carboxylates. 19 Over the past several decades, a plethora of both macrocyclic and nonmacrocyclic chelating ligands have been developed for a variety of radiometal ions.…”

Section: ■ Introductionmentioning

confidence: 99%

Octadentate Oxine-Armed Bispidine Ligand for Radiopharmaceutical Chemistry

et al. 2019

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In this study, we present the synthesis and characterization of the octadentate bispidine ligand, H2bispox2 and its complexes with medicinally useful radiometal nuclides (111In3+ and 177Lu3+), including their X-ray diffraction single crystal structures with the stable isotopes. 111InCl3 radiolabels the ligand quantitatively at ambient conditions ([L] = 10–5 M, room temperature, pH 7 and 15 min) and the in vitro human serum stability assays demonstrated high stability of the [111In(bispox2)]+ complex over 5 days. Moreover, the β ‑ emitter 177Lu radiolabels the ligand at 37 °C in 30 min (pH 8). These initial investigations reveal the potential of the octadentate bispidine ligand H2bispox2 as a useful chelator for 111In and 177Lu-based radiopharmaceuticals.

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