Positron emission tomography using 18F-labelled endothelin-1 reveals prevention of binding to cardiac receptors owing to tissue-specific clearance by ET B receptors in vivo

British Journal of Pharmacology

Volumn 144, Issue 1, 2005, Pages 115-122

  Johnström, Peter ^a   Fryer, Tim D ^a   Richards, Hugh K ^a   Harris, Neil G ^a   Barret, Olivier ^a   Clark, John C ^a   Pickard, John D ^a   Davenport, Anthony P ^a  

^a UNIVERSITY OF CAMBRIDGE   (United Kingdom)

Author keywords

18F; Endothelin; ET 1; In vivo imaging; MicroPET; PET; Positron emission tomography

Indexed keywords

ENDOTHELIN 1; ENDOTHELIN B RECEPTOR; ENDOTHELIN RECEPTOR; FLUORINE 18; HEART RECEPTOR; IODINE 125; N (2,6 DIMETHYLPIPERIDINOCARBONYL) 4 METHYLLEUCYL DEXTRO (1 METHOXYCARBONYLTRYPTOPHANYL) DEXTRO NORLEUCINE; RADIOLIGAND;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DRUG DISTRIBUTION; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; HEART LEFT VENTRICLE; HUMAN; HUMAN TISSUE; IMAGING SYSTEM; IN VIVO STUDY; INTERNALIZATION; ISOTOPE LABELING; ISOTOPE TRACING; KIDNEY; LIVER; LUNG; MALE; MEASUREMENT; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RAT; RECEPTOR DENSITY;

ANIMALS; ENDOTHELIN-1; FLUORINE RADIOISOTOPES; HEART VENTRICLES; HUMANS; MALE; POSITRON-EMISSION TOMOGRAPHY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, ENDOTHELIN; TISSUE DISTRIBUTION;

EID: 13244287739     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0706064     Document Type: Article

References (41)

1. 11C]L-753,037: studies in mice and a dog. J. Nucl. Med., 42, 1274-1280.
2. BREMNES, T., PAASCHE, J.D., MEHLUM, A., SANDBERG, C., BREMNES, B. & ATTRAMADAL, H. (2000). Regulation and intracellular trafficking pathways of the endothelin receptors. J. Biol. Chem., 275, 17596-17604.
3. CHATZIIOANNOU, A.F. (2002). Molecular imaging of small animals with dedicated PET tomographs. Eur. J. Nucl. Med. Mol. Imaging, 29, 98-114.
4. A receptor. J. Biol. Chem., 270, 10855-10860.
5. DAVENPORT, A.P. & KUC, R.E. (2002). Radioligand binding assays and quantitative autoradiography of endothelin receptors. Methods Mol. Biol., 206, 45-70.
6. DAVENPORT, A.P., MORTON, A.J. & BROWN, M.J. (1991). Localization of endothelin-1 (ET-1), ET-2, and ET-3, mouse VIC, and sarafotoxin S6b binding sites in mammalian heart and kidney. J. Cardiovasc. Pharmacol., 17 (Suppl 7), S152-S155.
7. DAVENPORT, A.P. & RUSSELL, F.D. (2001). Endothelin converting enzymes and endothelin receptor localisation in human tissues. In: Endothelin and its Inhibitors, ed. Warner, T.D., pp. 209-237. Berlin: Springer-Verlag.
8. DE NUCCI, G., THOMAS, R., DORLEANS-JUSTE, P., ANTUNES, E., WALDER, C., WARNER, T.D. & VANE, J.R. (1988). Pressor effects of circulating endothelin are limited by its removal in the pulmonary circulation and by the release of prostacyclin and endothelium-derived relaxing factor. Proc. Natl. Acad. Sci. U.S.A., 85, 9797-9800.
9. DUPUIS, J. (2000). Endothelin receptor antagonists and their developing role in cardiovascular therapeutics. Can. J. Cardiol., 16, 903-910.
10. B receptors. J. Appl. Physiol., 81, 1510-1515.
11. DUPUIS, J., SCHWAB, A.J., SIMARD, A., CERNACEK, P., STEWART, D.J. & GORESKY, C.A. (1999). Kinetics of endothelin-1 binding in the dog liver microcirculation in vivo. Am. J. Physiol., 277, G905-G914.
12. ERTL, G. & BAUERSACHS, J. (2004). Endothelin receptor antagonists in heart failure: current status and future directions. Drugs, 64, 1029-1040.
13. B receptors in rats. Biochem. Biophys. Res. Commun., 199, 1461-1465.
14. 125I]endothelin-1 by liver-derived cells. Arch. Biochem. Biophys., 305, 38-46.
15. GARDINER, S.M., KEMP, P.A. & BENNETT, T. (1993). Regional haemodynamic responses to intravenous and intraarterial endothelin-1 and big endothelin-1 in conscious rats. Br. J. Pharmacol., 110, 1532-1536.
16. B-receptor antagonist, on regional haemodynamic responses to endothelins in conscious rats. Br. J. Pharmacol., 112, 823-830.
17. 11,15]Ac-endothelin-1 (6-21) in conscious rats. Br. J. Pharmacol., 112, 477-486.
18. GELLAI, M., DEWOLF, R., PULLEN, M. & NAMBI, P. (1994). Distribution and functional role of renal ET receptor subtypes in normotensive and hypertensive rats. Kidney Int., 46, 1287-1294.
19. GIBSON, R.E., FIORAVANTI, C., FRANCIS, B. & BURNS, H.D. (1999). Radioiodinated endothelin-1: a radiotracer for imaging endothelin receptor distribution and occupancy. Nucl. Med. Biol., 26, 193-199.
20. HAYNES, W.G. & WEBB, D.J. (1998). Endothelin as a regulator of cardiovascular function in health and disease. J. Hypertens., 16, 1081-1098.
21. HOUSSET, C., ROCKEY, D.C. & BISSELL, D.M. (1993). Endothelin receptors in rat liver: lipocytes as a contractile target for endothelin 1. Proc. Natl. Acad. Sci. U.S.A., 90, 9266-9270.
22. ISHIKAWA, K., IHARA, M., NOGUCHI, K., MASE, T., MINO, N., SAEKI, T., FUKURODA, T., FUKAMI, T., OZAKI, S., NAGASE, T., NISHIKIBE, M. & YANO, M. (1994). Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proc. Natl. Acad. Sci. U.S.A., 91, 4892-4896.
23. JOHNSTRÖM, P., AIGBIRHIO, F.I., CLARK, J.C., DOWNEY, S.P.M.J., PICKARD, J.D. & DAVENPORT, A.P. (2000). Syntheses of the first endothelin-A- and -B-selective radioligands for positron emission tomography. J. Cardiovasc. Pharmacol., 36 (Suppl 1), S58-S60.
24. 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.
25. KALRA, P.R., MOON, J.C.C. & COATS, A.J.S. (2002). Do results of the ENABLE (endothelin antagonist bosentan for lowering cardiac events in heart failure) study spell the end for non-selective endothelin antagonism in heart failure? Int. J. Cardiol., 85, 195-197.
26. B in human kidney. Kidney Int., 44, 36-42.
27. KEDZIERSKI, R.M. & YANAGISAWA, M. (2001). Endothelin system: the double-edged sword in health and disease. Annu. Rev. Pharmacol. Toxicol., 41, 851-876.
28. KIMURA, S., KASUYA, Y., SAWAMURA, T., SHINMI, O., SUGITA, Y., YANAGISAWA, M., GOTO, K. & MASAKI, T. (1988). Structure-activity relationships of endothelin: importance of the C-terminal moiety. Biochem. Biophys. Res. Commun., 156, 1182-1186.
29. KINAHAN, P.E. & ROGERS, J.G. (1989). Analytic 3D image-reconstruction using all detected events. IEEE Trans. Nucl. Sci., 36, 964-968.
30. LEWIS, J.S., ACHILEFU, S., GARBOW, J.R., LAFOREST, R. & WELCH, M.J. (2002). Small animal imaging. Current technology and perspectives for oncological imaging. Eur. J. Cancer, 38, 2173-2188.
31. LÜSCHER, T.F. & BARTON, M. (2000). Endothelins and endothelin receptor antagonists: therapeutic considerations for a novel class of cardiovascular drugs. Circulation, 102, 2434-2440.
32. MARSAULT, R., FEOLDE, E. & FRELIN, C. (1993). Receptor externalization determines sustained contractile responses to endothelin-1 in the rat aorta. Am. J. Physiol., 264, C687-C693.
33. MIYAUCHI, T. & MASAKI, T. (1999). Pathophysiology of endothelin in the cardiovascular system. Annu. Rev. Physiol., 61, 391-415.
34. MOLENAAR, P., O'REILLY, G., SHARKEY, A., KUC, R.E., HARDING, D.P., PLUMPTON, C., GRESHAM, G.A. & DAVENPORT, A.P. (1993). Characterization and localization of endothelin receptor subtypes in the human atrioventricular conducting system and myocardium. Circ. Res., 72, 526-538.
35. OKSCHE, A., BOESE, G., HORSTMEYER, A., FURKERT, J., BEYERMANN, M., BIENERT, M. & ROSENTHAL, W. (2000). Late endosomal/ lysosomal targeting and lack of recycling of the ligand-occupied endothelin B receptor. Mol. Pharmacol., 57, 1104-1113.
36. PETER, M.G. & 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.
37. ROBB, R.A., HANSON, D.P., KARWOSKI, R.A., LARSON, A.G., WORKMAN, E.L. & STACY, M.C. (1989). Analyze: a comprehensive, operator-interactive software package for multidimensional medical image display and analysis. Comput. Med. Imaging Graph, 13, 433-454.
38. RUSSELL, F.D. & DAVENPORT, A.P. (1999). Secretory pathways in endothelin synthesis. Br. J. Pharmacol., 126, 391-398.
39. SCHIFFRIN, E.L., INTENGAN, H.D., THIBAULT, G. & TOUYZ, R.M. (1997). Clinical significance of endothelin in cardiovascular disease. Curr. Opin. Cardiol., 12, 354-367.
40. TAI, Y.C., CHATZIIOANNOU, A., SIEGEL, S., YOUNG, J., NEWPORT, D., GOBLE, R.N., NUTT, R.E. & CHERRY, S.R. (2001). Performance evaluation of the microPET P4: a PET system dedicated to animal imaging. Phys. Med. Biol., 46, 1845-1862.
41. WU-WONG, J.R. & OPGENORTH, T.J. (2001). The roles of endothelins in proliferations, apoptosis and angiogenesis. In: Endothelin and its Inhibitors, ed. Warner, T.D., pp. 299-322. Berlin: Springer-Verlag.