Nuclear Medicine and Biology
Volume 33, Issue 1 , Pages 15-19 , January 2006

Synthesis and in vivo evaluation of a PET radioligand for imaging the endothelin-A receptor

  • William B. Mathews

      Affiliations

    • Department of Radiology, Johns Hopkins Medical Institutions, Baltimore, MD 21287, USA
    • Corresponding Author InformationCorresponding author. Tel.: +1 410 614 0110; fax: +1 410 614 0111.
    • ,
  • Tamas G. Zober

      Affiliations

    • Department of Radiology, Johns Hopkins Medical Institutions, Baltimore, MD 21287, USA
    • ,
  • Hayden T. Ravert

      Affiliations

    • Department of Radiology, Johns Hopkins Medical Institutions, Baltimore, MD 21287, USA
    • ,
  • Ursula Scheffel

      Affiliations

    • Department of Radiology, Johns Hopkins Medical Institutions, Baltimore, MD 21287, USA
    • ,
  • John Hilton

      Affiliations

    • Department of Radiology, Johns Hopkins Medical Institutions, Baltimore, MD 21287, USA
    • ,
  • Darryl Sleep

      Affiliations

    • Abbott Laboratories, Abbott Park, IL 60064, USA
    • ,
  • Robert F. Dannals

      Affiliations

    • Department of Radiology, Johns Hopkins Medical Institutions, Baltimore, MD 21287, USA
    • ,
  • Zsolt Szabo

      Affiliations

    • Department of Radiology, Johns Hopkins Medical Institutions, Baltimore, MD 21287, USA

Received 7 February 2005 ,Revised 27 July 2005 ,Accepted 29 July 2005.

References 

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  2. Inoue A, Yanagisawa M, Kimura S, Kasuya Y, Miyauchi T, Goto K, et al. The human endothelin family: three structurally and pharmacologically distinct isopeptides predicted by three separate genes. Proc Natl Acad Sci U S A. 1989;86:2863–2867
  3. Wu-Wong JR, Opgenorth TJ. The roles of endothelins in proliferation, apoptosis, and angiogenesis. Handb Exp Pharmacol. 2001;152:299–322
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  6. Sakurai T, Yanagisawa M, Takuwa Y, Miyazaki H, Kimura S, Goto K, et al. Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor. Nature. 1990;348:732–735
  7. Moreau P, Dao HH. An update on the status of endothelin receptor antagonists for hypertension. Expert Opin Investig Drugs. 2001;10:1937–1946
  8. Luscher TF, Barton M. Endothelins and endothelin receptor antagonists: therapeutic considerations for a novel class of cardiovascular drugs. Circulation. 2000;102:2434–2440
  9. Seed A, Love MP, McMurray JJ. Clinical experience with endothelin receptor antagonists in chronic heart failure. Heart Fail Rev. 2001;6:317–323
  10. Bagnato A, Tecce R, Di Castro V, Catt KJ. Activation of mitogenic signaling by endothelin 1 in ovarian carcinoma cells. Cancer Res. 1997;57:1306–1311
  11. Kurbel S, Kurbel B, Kovacic D, Sulava D, Krajina Z, Dmitrovic B, et al. Endothelin-secreting tumors and the idea of the pseudoectopic hormone section in tumors. Med Hypotheses. 1999;52:329–333
  12. Brennan PA, Zaki GA. Angiogenesis in cancer: the role of endothelin-1. Ann R Coll Surg Engl. 2000;82:363–364
  13. Gibson RE, Fioravanti C, Francis B, Burns HD. Radioiodinated endothelin-1: a radiotracer for imaging endothelin receptor distribution and occupancy. Nucl Med Biol. 1999;26:193–199
  14. Johnström P, Harris NG, Fryer TD, Barret O, Clark JC, Pickard JD, et al. [18F]Endothelin-1, a positron emission tomography (PET) radioligand for the endothelin receptor system: radiosynthesis and in vivo imaging using microPET. Clin Sci. 2002;103(Suppl 48):4S–8S
  15. Ravert HT, Mathews WB, Hamill TG, Burns HD, Dannals RF. Radiosynthesis of a potent endothelin receptor antagonist: [11C]L-753,037. J Label Comp Radiopharm. 2000;43:1205–1210
  16. Aleksic S, Szabo Z, Scheffel U, Ravert HT, Mathews WB, Kerenyi L, et al. In vivo labeling of endothelin receptors with [11C]L-753,037: studies in mice and a dog. J Nucl Med. 2001;42:1274–1280
  17. Johnström P, Aigbirhio FI, Clark JC, Downey SP, Pickard JD, Davenport AP. Syntheses of the first endothelin-A- and -B-selective radioligands for positron emission tomography. J Cardiovasc Pharmacol. 2000;36:S58–S60
  18. Winn M, von Geldern TW, Opgenorth TJ, Jae HS, Tasker AS, Boyd SA, et al. 2,4-Diarylpyrrolidine-3-carboxylic acids-potent ETA selective endothelin receptor antagonists: 1. Discovery of A-127722. J Med Chem. 1996;39:1039–1048
  19. Hilton J, Yokoi F, Dannals RF, Ravert HT, Szabo Z, Wong DF. Column-switching HPLC for the analysis of plasma in PET imaging studies. Nucl Med Biol. 2000;27:627–630

PII: S0969-8051(05)00201-5

doi: 10.1016/j.nucmedbio.2005.07.012

Nuclear Medicine and Biology
Volume 33, Issue 1 , Pages 15-19 , January 2006

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