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Imaging and Characterization of Radioligands for Positron Emission Tomography Using Quantitative Phosphor Imaging Autoradiography

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Receptor Binding Techniques

Part of the book series: Methods in Molecular Biology™ ((MIMB,volume 306))

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Abstract

Quantification of radioligand binding by exposing labeled tissue sections to phosphor screens in cassettes is similar to autoradiography using radiation sensitive film (1) (see Chapters 5 and 7). The major advantage of phosphor screens over film is the greatly increased sensitivity with exposure times reduced by at least one order of magnitude (2,3). This is essential for short-lived radionuclides—such as 18F and 111C, with half-lives of 109.8 and 20.4 min, respectively—that are used to label peptide or drug ligands to image receptors noninvasively in vivo by positron emission tomography (PET) (see Chapter 11). Phosphor imaging can also considerably reduce exposure times for weak β-particle emitters such as 3H from months to days (3). A second advantage is the increased linear dynamic range of five orders of magnitude (2,3). This increased dynamic range makes it less likely that screens will be saturated. This is important for PET radioligands in which, owing to the short half-life of the radionuclide, it is only possible to image once, whereas re-exposure is possible for isotopes with longer half-lives.

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References

  1. Davenport, A.P. (2000) Endothelin receptors. IUPHAR Compendium of Receptor Characterisation and Classification, 2nd Edition. IUPHAR Media, London, UK: 182–188.

    Google Scholar 

  2. Johnston, R.F., Pickett, S.C., and Barker, D.L. (1990) Autoradiography using storage phosphor technology. Electrophoresis 11, 355–360.

    Article  PubMed  CAS  Google Scholar 

  3. Upham, L.V. and Englert, D.F. (1998) Radionuclide imaging. In Handbook of Radioactivity Analysis (LA’nnunziata, M. F., ed.). Academic, San Diego, CA: pp. 647–692.

    Google Scholar 

  4. Chen, S.-F., Richards, H. K., Smielewski, P., et al. (2004) Relationship between flow-metabolism uncoupling and evolving axonal injury after experimental traumatic brain injury. J. Cereb. Blood Flow Metab., 24, 1025–1036.

    Article  PubMed  CAS  Google Scholar 

  5. Johnström, P., Harris, N. G., Fryer, T. D., et al. (2002) 18F-Endothelin-1, a positron emission tomography (PET) radioligand for the endothelin receptor system: radiosynthesis and in vivo imaging using microPET. Clin. Sci. 103(Suppl 48), 4S–8S.

    PubMed  Google Scholar 

  6. Johnström, P., Fryer, T. D., Richards, H.K, et al. (2004). Positron emission tomography using 18F-labelled endothelin-1 reveals prevention of binding to cardiac receptors owing to tissue-specific clearance by ETB receptors in vivo. Br. J. Pharmacol. 144, 115–122.

    Article  Google Scholar 

  7. Sihver W., Sihver, S., Bergström, M., et al. (1997) Methodological aspects for in vitro characterisation of receptor binding using 11C-labeled receptor ligands: a detailed study with the benzodiazepine receptor antagonist [1 1C]Ro 15–1788. Nucl Med.Biol. 24, 723–731.

    Article  PubMed  CAS  Google Scholar 

  8. Peter, M. G. and Davenport, A. P. (1996) Characterization of the endothelin receptor selective agonist, BQ3020 and antagonists BQ123, FR139317, BQ788, 50235, Ro462005 and bosentan in the heart. Br. J. Pharmacol. 117, 455–462.

    PubMed  CAS  Google Scholar 

  9. Karet, F. E., Kuc, R E. and Davenport, A. P. (1993) Novel ligands BQ123 and BQ3020 characterize endothelin receptor subtypes ETA and ETB in human tissue. Kidney Int. 44, 36–42.

    Article  PubMed  CAS  Google Scholar 

  10. Munson, P. J. and Rodbard, D. (1980) Ligand: a versatile computerized approach for characterization of ligand-binding systems. Anal. Biochem. 107, 220–239.

    Article  PubMed  CAS  Google Scholar 

  11. McPherson, G. A. (1985) Analysis of radioligand binding experiments. A collection of computer programs for the IBM PC. J. Pharmacol. Methods 14, 213–228.

    Article  PubMed  CAS  Google Scholar 

  12. Reinprecht, I., Windisch, M., and Fahnestock, M. (2002) Deterioration of storage phosphor screens with use. J. Label. Compd. Radiopharm. 45, 339–345.

    Article  CAS  Google Scholar 

  13. Sihver, S., Sihver, W., Bergström, M., et al. (1999) Quantitative autoradiography with short-lived positron emission tomography tracers: a study on muscarinic ace tylcholine receptors with N-[(si11)C]-4-piperidylbenzilate. J. Pharmacol. Exp. Ther. 290, 917–922.

    PubMed  CAS  Google Scholar 

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JohnstrÖm, P., Davenport, A.P. (2005). Imaging and Characterization of Radioligands for Positron Emission Tomography Using Quantitative Phosphor Imaging Autoradiography. In: Davenport, A.P. (eds) Receptor Binding Techniques. Methods in Molecular Biology™, vol 306. Humana Press. https://doi.org/10.1385/1-59259-927-3:203

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  • DOI: https://doi.org/10.1385/1-59259-927-3:203

  • Publisher Name: Humana Press

  • Print ISBN: 978-1-58829-420-3

  • Online ISBN: 978-1-59259-927-1

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