Technetium-99m-Labeled HOE 140: A Potential Bradykinin B2 Receptor Imaging Agent

Stahl, Wilhelm; Breipohl, Gerhard; Kuhlmann, L.; Steinsträsser, A; Hj, Gerhards; Ba, Schölkens

doi:10.1021/jm00015a001

Cited by 9 publications

(7 citation statements)

References 2 publications

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“…HOE 140 has been labelled with 99m Tc using CPTA (4-[(1,4,8,11-tetraazacyclotetradecane-1-yl)methyl]benzoic acid) as a bifunctional chelating agent (61). 112 At pH 10, greater than 95% complexation was achieved after 10 minutes using tin(II) citrate and sodium [ 99m Tc]pertechnetate(VII). The biodistribution data showed no enrichment of any specific organ except liver and kidney, which are important for the excretion of 99m Tc-labelled CPTA-HOE 140.…”

Section: Peptide Pharmaceuticals Some Specifically-targetedmentioning

confidence: 99%

Cyclam complexes and their applications in medicine

2004

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Cyclams are 14-membered tetraamine macrocycles which bind strongly to a wide range of metal ions. Medical interest has centred on clinical trials of a bicyclam for the treatment of AIDS and for stem cell mobilization, and on adducts with Tc and Cu radionuclides for diagnosis and therapy. Other potential applications particularly for Cr, Mn, Zn, and Ru cyclams are also emerging. We discuss in this critical review the mechanism of metal complexation, stability of metal cyclams and their structures, with particular emphasis on the variety of configurational states which metal cyclams can adopt. Understanding the factors which control the thermodynamics and kinetics of the interconversion of configurational states of metallo-cyclams may be a key factor in designing novel cyclam derivatives for future use in medicine.

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Section: Peptide Pharmaceuticals Some Specifically-targetedmentioning

confidence: 99%

Cyclam complexes and their applications in medicine

2004

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“…Although fluorescent derivatives have been reported for microscopy and flow cytometry (10,11), there have been so far few successful attempts to visualize B1R-expressing tissues noninvasively, in vivo. Stahl and colleagues described a 99m Tc-labeled peptide (HOE 140) to visualize B2R expression, and evaluated the biodistribution of this compound in healthy mice (12). Fuchs and colleagues reported the visualization of chronic cutaneous delayed type hypersensitivity reaction in mice using a 11 C-labeled sulfonamide targeting B1R, but high, nondisplaceable background activity was observed with the radiotracer (13).…”

Section: Introductionmentioning

confidence: 99%

In Vivo Radioimaging of Bradykinin Receptor B1, a Widely Overexpressed Molecule in Human Cancer

et al. 2015

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The bradykinin receptor B1R is overexpressed in many human cancers where it might be used as a general target for cancer imaging. In this study, we evaluated the feasibility of using radiolabeled kallidin derivatives to visualize B1R expression in a preclinical model of B1R-positive tumors. Three synthetic derivatives were evaluated in vitro and in vivo for receptor binding and their ability to visualize tumors by PET. Enalaprilat and phosphoramidon were used to evaluate the impact of peptidases on tumor visualization. While we found that radiolabeled peptides based on the native kallidin sequence were ineffective at visualizing B1R-positive tumors, peptidase inhibition with phosphoramidon greatly enhanced B1R visualization in vivo. Two stabilized derivatives incorporating unnatural amino acids ( 68 Ga-SH01078 and 68 Ga-P03034) maintained receptor-binding affinities that were effective, allowing excellent tumor visualization, minimal accumulation in normal tissues, and rapid renal clearance. Tumor uptake was blocked in the presence of excess competitor, confirming that the specificity of tumor accumulation was receptor mediated. Our results offer a preclinical proof of concept for noninvasive B1R detection by PET imaging as a general tool to visualize many human cancers.

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“…173 Despite early reports indicating that cyclam is an efficient chelating agent for 99m Tc, 174,175 the subsequent use of bifunctional cyclam agents (such as CPTA 176 ) in 99m Tc radiolabelling applications reveals quite low radiolabelling efficiency at physiological conditions, often requiring highly The binuclear 99m Tc complex of AMD3100 was evaluated by basic conditions (pH ¼ 10) to achieve higher labelling yields. 177,178 Encouragingly, in this preliminary study, the radiolabelling reaction was high yielding (98.5 AE 1.2%) under mild reaction conditions. In addition, this radiotracer was shown to be very stable in both PBS (pH 7.4) and HAS at room temperature.…”

Section: Radiolabelled Small Moleculesmentioning

confidence: 59%

Nuclear (PET/SPECT) and optical imaging probes targeting the CXCR4 chemokine receptor

Knight

Wuest

2012

Med. Chem. Commun.

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The chemokine receptor CXCR4 has been found to be highly expressed in a wide variety of cancer types, including breast, colorectal, melanoma, nasopharyngeal, oesophageal, osteosarcoma, and nonsmall-cell lung carcinoma. It has been shown that these elevated expression levels are yet further increased upon metastasis. This receptor therefore represents a highly attractive target which could facilitate the diagnostic imaging of many aggressive cancers. Since 2005, there have been a wide assortment of CXCR4-targeting imaging probes spanning both nuclear (PET/SPECT) and optical imaging modalities. This review highlights a wide variety of pertinent examples from the recent literature, placing special focus on the chemical aspects of probe design. James C: Knight Dr James C. Knight obtained a BSc in chemistry from Cardiff University in 2005 and subsequently a PhD in 2009 under the supervision of Dr Angelo J. Amoroso and Prof. Peter G. Edwards. He subsequently spent two years working between the Cardiff School of Biosciences and Chemistry departments developing multimodal imaging agents under the supervision of

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Technetium-99m-Labeled HOE 140: A Potential Bradykinin B2 Receptor Imaging Agent

Cited by 9 publications

References 2 publications

Cyclam complexes and their applications in medicine

Cyclam complexes and their applications in medicine

In Vivo Radioimaging of Bradykinin Receptor B1, a Widely Overexpressed Molecule in Human Cancer

Nuclear (PET/SPECT) and optical imaging probes targeting the CXCR4 chemokine receptor

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