Synthesis and Cardiac Imaging of <sup>18</sup>F-Ligands Selective for β<sub>1</sub>-Adrenoreceptors

Radeke, Heike; Purohit, Ajay; Harris, Thomas D.; Hanson, Kelley; Jones, Reinaldo; Hu, Carol; Yalamanchili, Padmaja; Hayes, Megan; Yu, Ming; Guaraldi, Mary; Kagan, Mikhail; Azure, Michael; Cdebaca, Michael; Robinson, Simon P.; Casebier, David S.

doi:10.1021/ml1002458

Cited by 9 publications

(6 citation statements)

References 23 publications

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“…However, accomplishments in this field have been scarce in the past decade, partially due to the low selectivity towards mAChRs shown by the probes developed [125,126,127,128,129]. A few PET probes for targeting specific adrenoreceptor subtypes have also been designed and assessed for cardiac [130,131,132] or brain [133,134,135] molecular imaging.…”

Section: Introductionmentioning

confidence: 99%

Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics

et al. 2018

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Precision medicine relies on individually tailored therapeutic intervention taking into account individual variability. It is strongly dependent on the availability of target-specific drugs and/or imaging agents that recognize molecular targets and patient-specific disease mechanisms. The most sensitive molecular imaging modalities, Single Photon Emission Computed Tomography (SPECT) and Positron Emission Tomography (PET), rely on the interaction between an imaging radioprobe and a target. Moreover, the use of target-specific molecular tools for both diagnostics and therapy, theranostic agents, represent an established methodology in nuclear medicine that is assuming an increasingly important role in precision medicine. The design of innovative imaging and/or theranostic agents is key for further accomplishments in the field. G-protein-coupled receptors (GPCRs), apart from being highly relevant drug targets, have also been largely exploited as molecular targets for non-invasive imaging and/or systemic radiotherapy of various diseases. Herein, we will discuss recent efforts towards the development of innovative imaging and/or theranostic agents targeting selected emergent GPCRs, namely the Frizzled receptor (FZD), Ghrelin receptor (GHSR-1a), G protein-coupled estrogen receptor (GPER), and Sphingosine-1-phosphate receptor (S1PR). The pharmacological and clinical relevance will be highlighted, giving particular attention to the studies on the synthesis and characterization of targeted molecular imaging agents, biological evaluation, and potential clinical applications in oncology and non-oncology diseases. Whenever relevant, supporting computational studies will be also discussed.

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Section: Introductionmentioning

confidence: 99%

Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics

et al. 2018

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“…The indirect labeling approach based on the synthesis and purification of [ 18 F]FETs followed by [ 18 97 MedChemComm Review ICI 89 406. 101 In that publication, the average overall RCY for [ 18 F]fluoroalkylation using the indirect method was 30%. Also, in this example, the direct labeling process using the corresponding tosylate precursors demonstrated a rather poor chemical efficiency (<2% radiochemical yield).…”

Section: Direct Versus Indirect Radiolabelingmentioning

confidence: 98%

2-[¹⁸F]Fluoroethyl tosylate – a versatile tool for building¹⁸F-based radiotracers for positron emission tomography

et al. 2015

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“…3 were synthesised by O-alkylation of the phenolic precursor with 150. 49,68,80,89,99,100,[137][138][139][140] The alkylation reactions were performed in DMSO, DMF or MeCN at around 100 1C and different bases were employed (NaH, NaOH, K 2 CO 3 or TBAOH). The precursor of the serotonin transporter ligand 167 was pre-incubated with the base prior to [ 18 F]fluoropropylation to form the phenolate, thereby facilitating nucleophilic substitution.…”

Section: [ 18 F]fluoroformmentioning

confidence: 99%

Fluorine-18 labelled building blocks for PET tracer synthesis

et al. 2017

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Positron emission tomography (PET) is an important driver for present day healthcare. Fluorine-18 is the most widely used radioisotope for PET imaging and a thorough overview of the available radiochemistry methodology is a prerequisite for selection of a synthetic approach for new fluorine-18 labelled PET tracers. These PET tracers can be synthesised either by late-stage radiofluorination, introducing fluorine-18 in the last step of the synthesis, or by a building block approach (also called modular build-up approach), introducing fluorine-18 in a fast and efficient manner in a building block, which is reacted further in one or multiple reaction steps to form the PET tracer. This review presents a comprehensive overview of the synthesis and application of fluorine-18 labelled building blocks since 2010.

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Synthesis and Cardiac Imaging of ¹⁸F-Ligands Selective for β₁-Adrenoreceptors

Cited by 9 publications

References 23 publications

Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics

Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics

2-[¹⁸F]Fluoroethyl tosylate – a versatile tool for building¹⁸F-based radiotracers for positron emission tomography

Fluorine-18 labelled building blocks for PET tracer synthesis

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Synthesis and Cardiac Imaging of 18F-Ligands Selective for β1-Adrenoreceptors

Cited by 9 publications

References 23 publications

Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics

Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics

2-[18F]Fluoroethyl tosylate – a versatile tool for building18F-based radiotracers for positron emission tomography

Fluorine-18 labelled building blocks for PET tracer synthesis

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Product

Resources

About

Synthesis and Cardiac Imaging of ¹⁸F-Ligands Selective for β₁-Adrenoreceptors

2-[¹⁸F]Fluoroethyl tosylate – a versatile tool for building¹⁸F-based radiotracers for positron emission tomography