New amino bisphosphonate compound for skeletal imaging: Comparison study with methylenediphosphonic acid (MDP) and (1-hydroxyethane-1,1-diyl) diphosphonic acid (HEDP)

• Autorzy: Assaad T.

Identyfikatory

DOI

10.1515/nuka-2016-0013

• Języki publikacji: EN

Abstrakty

EN

A novel bisphosphonate derivative (1-aminoethane-1,1-diyl)diphosphonic acid (AEDP) has been prepared and successfully labeled with 99mTc at high labeling yields. The in vivo biodistribution of 99mTc-AEDP has been investigated and compared with two reference compounds Tc-99m methylene diphosphonate (99mTc-MDP) and Tc-99m (1-hydroxyethylidene) diphosphonate (99mTc-HEDP). The biodistribution studies have demonstrated a high uptake of the radiotracer 99mTc-AEDP in the bone and a rapid clearance from the blood (such as the two technetium-labeled bone imaging agents in current use: 99mTc-MDP and 99mTc-HEDP). Additionally, the scintigraphic images of 99mTc-AEDP in normal rats have revealed high selective skeletal uptake.

Słowa kluczowe

EN

aminoethylidenediphosphonic acid; biodistribution; bisphosphonates; bone imaging agent; radiolabeling

• Wydawca: Institute of Nuclear Chemistry and Technology
• Czasopismo: Nukleonika
• Rocznik: 2016
• Tom: Vol. 61, No. 1
• Strony: 69--74
• Opis fizyczny: Bibliogr. 16 poz., rys.

Twórcy

autor

Assaad T.

• T. Assaad Radioisotopes Division, Radioisotopes Department, Atomic Energy Commission of Syria (AECS), P. O. Box 6091, Damascus, Syrian Arab Republic, Tel.: [phone], Fax: [phone]

Bibliografia

• 1. Jurisson, S., & Lydon, S. (1999). Potential technetium small molecule radiopharmaceuticals. Chem. Rev., 99(9), 2205–2218. DOI: 10.1021/cr980435t.
• 2. Fleisch, H. A. (1998). Bisphosphonates: mechanisms of action. Endocr. Rev., 19(1), 80–100.
• 3. Papapoulos, S. E. (1995). Pharmacodynamics of bisphosphonates in man. In O. Bijvoet, H. Fleisch, R. E. Comfield, & G. G. Russell (Eds.), Bisphosphates on bone (Chapter 15). Amsterdam: Elsevier Science B.V.
• 4. Subramanian, G., McAfee, J. G., Blair, R. J., Kallfelz, F. A., & Thomas, F. D. J. (1975). Technetium-99m--methylene diphosphonate – a superior agent for skeletal imaging: comparison with other technetium complexes. J. Nucl. Med., 16(8), 744–755. DOI: 10.2174/092986712801215865.
• 5. Bevan, J. A., Tofe, A. J., Benedict, J. J., Francis, M. D., & Barnett, B. L. (1980). Tc-99m HMDP (HydroxymethyleneDiphosphonate): A radiopharmaceutical for skeletal and acute myocardial infarct imaging. I. Synthesis and distribution in animals. J. Nucl. Med., 21(10), 961–966. DOI: 10.2174/092986712801215865.
• 6. Bartholoma, M. D., Louie, A. S., Valliant, J. F., & Zubieta, J. (2010). Technetium and gallium derived radiopharmaceuticals: comparing and contrasting the chemistry of two important radiometals for the molecular imaging era. J. Chem. Rev., 110(5), 2903–2920. DOI: 10.1021/cr1000755.
• 7. Russell, R. G. G., & Fleisch, H. (1975). Pyrophosphate and diphosphonates in skeletal metabolism. Clin. Orthop., 108, 241–263.
• 8. Shinoda, H., Adamek, G., Felix, R., Fleisch, H., Schenk, R., & Hagan, P. (1983). Structure-activity relationships of various bisphosphonates. Calcif. Tissue Int., 35, 87–99. DOI: 10.1007/BF02405012.
• 9. Schenk, R., Eggli, P., Fleisch, H., & Rosini, S. (1986). Quantitative morphometric evaluation of the inhibitory activity of new. Amino bisphosphonates on bone resorption in the rat. Calcif. Tissue Int., 38, 342–349. DOI: 10.1007/BF02555748.
• 10. Pluijm, G. V. D., Binderup, L., Bramm, E., Wee-Pals, L. V. D., Groot, H. D., & Binderup, E. (1992). Disodium 1-hydroxy-3-(1-pyrrolidinyl)-propylidene-1,1--bisphosphonate (EB-1053) is a potent inhibitor of bone resorption in vitro and in vivo. J. Bone Miner. Res., 7, 981–986. DOI: 10.1002/jbmr.5650070815.
• 11. Sato, M., & Grasser, W. (1990). Effects of bisphosphonates on isolated rat osteoclasts as examined by reflected light microscopy. J. Bone Miner. Res., 5, 31–40. DOI: 10.1002/jbmr.5650050107.
• 12. Rudd, T. G., Allen, D. R., & Hartnett, D. E. (1977). Tc-99m methylene diphosphonate versus Tc-99m pyrophosphate: biologic and clinical comparison. J.Nucl. Med., 18, 872–876.
• 13. Lin, W. Y., & Wang, S. J. (1996). The infl uence of two bone agents (Tc-99m pyrophosphate and Tc-99m methylenediphosphonate) on quantitative sacroiliac joint scintigraphy. Nucl. Med. Commun., 17, 1035–1038.
• 14. Imanishi, Y., Mitogawa, Y., Takizawa, M., Konno, S., Samura, H., & Ohsawa, A. (1999). Relapsing polychondritis diagnosed by Tc-99m MDP bone scintigraphy. Clin. Nucl. Med., 24, 511–513.
• 15. Altomare, A., Cuocci, C., Giacovazzo, C., Moliterni, A., & Rizzi, R. (2008). A computer program for qualitative analysis using powder diffraction data. J. Appl. Cryst., 41, 815–817. DOI: 10.1107/S0021889808016956.
• 16. Tsaryk, N. V., Dudko, A. V., Kozachkova, A. N., &Pekhnyo, V. I. (2011). A second triclinic polymorph of (1-ammonio-1-phosphono eth yl)phosphonate. Acta Crystallogr. Sect. E-Struc. Rep. Online, 67, o1651–o1652. DOI: 10.1107/S1600536811022239.

Uwagi

PL

Opracowanie ze środków MNiSW w ramach umowy 812/P-DUN/2016 na działalność upowszechniającą naukę.