Artikel
Lizenziert
Nicht lizenziert Erfordert eine Authentifizierung

Radiocomplexation and bioevaluation of 99mTc nitrido-piracetam as a model for brain imaging

  • EMAIL logo , und
Veröffentlicht/Copyright: 19. April 2017
Radiochimica Acta
Aus der Zeitschrift Radiochimica Acta Band 105 Heft 9

Abstract

The aim of the work is to radiolabel a piracetam using [99mTc≡N]2+core in order to give a 99mTcN-labeled piracetam complex, that is expected to concentrate in brain organ by AMPA receptors. The complex was prepared with high radiochemical purity (>98.0) and maintained stability throughout the working period (8 h) using different quality controls. Biodistribution investigation showed that, the maximum uptake of the complex in the brain was 13.5±0.12% at 5 min post injection (p.i.) of the injected dose/g which retained till 2 h post-injection.

Keywords: Piracetam; [99mTc≡N]2+core; labeling; biodistribution; brain; imaging

Acknowledgments

The authors would like to express our deep gratitude and sincere appreciation to Prof. Dr. E.H.Borai for sincere efforts in reviewing and helping us in our answered to reviewers questions.

References

1. Filler, A. F.: The history, development and impact of computed imaging in neurological diagnosis and neurosurgery: CT, MRI, and DTI. Int. J. Neurosurg. 7(1), 5 (2010).10.5580/23c6Suche in Google Scholar

2. Sandrone, S., Bacigaluppi, M., Galloni, M. R., Cappa, S. F., Moro, A., Catani, M., Filippi, M., Monti, M. M., Perani, D., Martino, G.: Weighing brain activity with the balance: Angelo Mosso’s original manuscripts come to light. Brain. 137(2), 621 (2014).10.1093/brain/awt091Suche in Google Scholar PubMed

3. Peruzzotti-Jametti, L., Bacigaluppi, M., Sandrone, S., Cambiaghi, M.: Emerging subspecialties in Neurology: transcranial stimulation. Neurology. 80(4), e33 (2013).10.1212/WNL.0b013e3182833d74Suche in Google Scholar PubMed

4. Martino, G., Bacigaluppi, M.: Mechanism of action of somatic stem cell treatments: towards the concept of therapeutic plasticity. Cytotherapy. 13(1), 6 (2011).10.3109/14653249.2011.537055Suche in Google Scholar PubMed

5. Butti, E., Cusimano, M., Bacigaluppi, M., Martino, G.: Neurogenic and non-neurogenic functions of endogenous neural stem cells. Front Neurosci 8, 92 (2014).10.3389/fnins.2014.00092Suche in Google Scholar PubMed PubMed Central

6. Chang, C., Shiau, Y., Wang, J., Ho, S., Kao, A.: Abnormal regional cerebral blood flow on 99mTc ECD brain SPECT in patients with primary Sjögren’s syndrome and normal findings on brain magnetic resonance imaging. Ann. Rheum. Dis. 61, 774 (2002).10.1136/ard.61.9.774Suche in Google Scholar PubMed PubMed Central

7. Ogasawara, K., Ogawa, A., Ezura, M., Konno, H., Suzuki, M., Yoshimoto, T.: Brain ingle-photon emission CT studies using 99mTc-HMPAO and 99mTc-ECD early after recanalization by local intraarterial thrombolysis in patients with acute embolic middle cerebral artery occlusion. Am. J. Neuroradiol. 22, 48 (2001).Suche in Google Scholar

8. Wong, D. F., Gründer, G., Brasic, J. R.: Brain imaging research: does the science serve clinical practice? Int. Rev. Psychiatr. 19(5), 541 (2007).10.1080/09540260701564849Suche in Google Scholar PubMed

9. Malykh, A. G., Sadaie, M. R.: Piracetam and piracetam-like drugs: from basic science to novel clinical applications to CNS disorders. Drugs. 70(3), 287 (2010).10.2165/11319230-000000000-00000Suche in Google Scholar PubMed

10. Stensbol, T. B., Madsen, U., Krogsgaard-Larsen, P.: The AMPA receptor site: focus on agonists and competitive antagonists. Curr. Pharm. Des. 8(10), 857 (2002).10.2174/1381612024607090Suche in Google Scholar PubMed

11. Amin, A., Sanad, M. H., Abd-Elhaliem, S.: Radiochemical and biological characterization of 99mTc-piracetam for brain imaging. Radiochemistry. 55, 624 (2013).10.1134/S1066362213060118Suche in Google Scholar

12. Syed, Q. S., Mohammad, R. K., Syed, M. A.: Radiosynthesis of 99mTc (CO)3-clinafloxacin dithiocarbamate and its biological evaluation as a potential staphylococcus aureus infection radiotracer. Nucl. Med. Mol. Imaging. 45, 248 (2011).10.1007/s13139-011-0106-8Suche in Google Scholar PubMed PubMed Central

13. Mohini, G., Subhajit, G., Tapas, D., Haladhar, D. S. S. B.: Preparation and bioevaluation of [99mTc≡N]2+ labeled tetrameric complex of E c(RGDfK)2 as a radiotracer for imaging avb3 integrins in tumors. J. Radioanal. Nucl. Chem. 309, 923 (2016).Suche in Google Scholar

14. Mingxia, Z., Hongyu, N., Man, F., Shilei, L., Jin, C., Chuanmin Q.: Novel [99mTc≡N]2 labeled EGFR inhibitors as potential radiotracers for single photon emission computed tomography (SPECT) tumor imaging. Molecules. 19, 5508 (2014).10.3390/molecules19055508Suche in Google Scholar

15. Xiang, L., Aiqin, W., Qianqian, X., Yu, F., Jianping, L., Huabei, Z., Huaying, B.: Synthesis and biological evaluation of fatty acids containing 99mTc-oxo and 99mTc-nitrido for myocardial metabolism imaging. J. Radioanal. Nucl. Chem. 307, 1438 (2016).10.1007/s10967-015-4232-0Suche in Google Scholar

16. Adrion, D., Alessandra, B., Licia, U.: Technetium -99m Nitrido-radiopharmaceuticals with un precedented biological properties. Braz. Arch. Biol. Techn. 45, 135 (2002).10.1590/S1516-89132002000500019Suche in Google Scholar

17. Alessandra, B., Licia, U., Cristina, B., Adriano, D., Nicola, S., Elena, M., Giovanni, D. D., Guido, Z., Fiorenzo, R., Melchiore G.: Synthesis and biologic evaluation of monocationic asymmetric 99mTc-nitride heterocomplexes showing high heart uptake and improved imaging properties. J. Nucl. Med. 44(5), 806 (2003).Suche in Google Scholar

18. Ardhani, D. L., Andi, T. P., Tini, P., Evi, U., Mochammad, Y., Gunawan, I.: HPLC determination of piracetam in tablets; validation of the method. J. Liq. Chromatogr. R. T. 28(9), 1407 (2007).10.1081/JLC-200054893Suche in Google Scholar

19. Sanad, M. H.: Novel radiochemical and biological characterization of 99mTc-histamine as a model for brain imaging. J. Anal. Sci. Technol. 5(1), 23 (2014).10.1186/s40543-014-0023-4Suche in Google Scholar

20. Sanad, M. H.: Labeling of omeprazole with technetium-99m for diagnosis of stomach. Radiochemistry. 55, 605 (2013).10.1134/S1066362213060076Suche in Google Scholar

21. Sanad, M. H., El-Bayoumy, A. S. A., Alhussein, A. I.: Comparative biological evaluation between 99mTc(CO)3 and 99mTc-Sn (II) complexes of novel quinoline derivative: a promising infection radiotracer. J. Radioanal. Nucl. Chem. 31, 1 (2017).10.1007/s10967-016-4945-8Suche in Google Scholar

22. Sanad, M. H.: Labeling and biological evaluation of 99mTc-azithromycin for Infective inflammation diagnosis. Radiochemistry. 55(5), 539 (2013).10.1134/S1066362213050159Suche in Google Scholar

23. Rhodes, B. A.: Considerations in the radiolabeling of albumin. Semin. Nucl. Med. 4(3), 281 (1974).10.1016/S0001-2998(74)80015-2Suche in Google Scholar

24. Amin, A. M., El-Azony, K. M., Ibrahim, I. T.: Application of 99Mo/99mTc alumina generator in the labeling of metoprolol for diagnostic purposes. J. Label. Compd. Radiopharm. 52(11), 467 (2009).10.1002/jlcr.1661Suche in Google Scholar

25. Ahmed, A. H., Oswald, R. E.: Piracetam defines a new binding site for allosteric modulators of α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptors. J. Med. Chem. 53(5), 2197 (2010).10.1021/jm901905jSuche in Google Scholar PubMed PubMed Central

26. Anupam, M., Madhava, B. M., Suresh, S., Sharmila, B., Kothari, K., Bhaskar, D., Sarmad, H. D., Meera, V.: 99mTcN complexes of tert-butyl dithiocarbamate and methoxyisobutyl dithiocarbamate as myocardial and brain imaging agents. Nucl. Med. Commun. 26, 1013 (2005).10.1097/01.mnm.0000183793.51474.2fSuche in Google Scholar

27. Sanad, M. H., Borai, E. H.: Comparative biological evaluation between 99mTc tricarbonyl and 99mTc-Sn (II) levosalbutamol as a β2-adrenoceptor agonist. Radiochim. Acta. 103(12), 879 (2015).10.1515/ract-2015-2428Suche in Google Scholar

28. Bonte, F. J., Hynan, L., Harris, T. S., White, C. L.: 99mT -HMPAO brain blood flow imaging in the dementias with histopathologic correlation in 73 patients. J. Mol. Imaging. ID 2011, 409101 (2011).10.1155/2011/409101Suche in Google Scholar

29. Brooks, D. J.: Positron emission tomography and single-photon emission computed tomography in central nervous system drug development. NeuroRx 2(2), 226 (2005).10.1602/neurorx.2.2.226Suche in Google Scholar

30. Neirinckx, R. D., Canning, L. R., Piper, I. M., Nowotnik, D. P., Pickett, R. D., Holmes, R. A., Volkert, W. A., Forster, A. M., Weisner, P. S., Marriott, J. A., Chaplin, S. B.: 99mT – D,L HMPAO a new radiopharmaceutical for SPECT imaging of regional cerebral blood flow. J. Nucl. Med. 28, 191 (1987).Suche in Google Scholar

31. Walovitch, R. C., Hill, T. C., Garrity, S. T., Cheesman, E. H., Burgess, B. A., O’Leary, D. H., Watson, A. D., Ganey, M. V., Morgan, R. A., Williams, S. J.: Characterization of 99mTc-l,l-ECD for brain perfusion imaging. Part 1: pharmacology of 99mTc-ECD in non-human primates. J. Nucl. Med. 30, 1892 (1989).Suche in Google Scholar

32. Sanad, M. H., Ibrahim, I.: Radiodiagnosis of peptic ulcer with technetium-99m labeled rabeprazole. J. Radiochemistry 57, 425 (2015).10.1134/S1066362215040165Suche in Google Scholar

33. Sanad, M. H., Sakr, T. M., Walaa, H. A. A., Marzook, E. A.: In silico study and biological evaluation of 99mTc-tricabonyl oxiracetam as a selective imaging probe for AMPA receptors. J. Radioanal. Nucl. Chem. DOI 10.1007/s10967-016-5120-y (2016).10.1007/s10967-016-5120-ySuche in Google Scholar

34. Satpati, D., Bapat, K., Mukherjee, A., Banerjee, S., Kothari, K., Venkatesh, M.: Preparation and bioevaluation of 99mTc-carbonyl complex of 5-hydroxy tryptamine derivative. Appl. Rad. Isot. 64(8), 888 (2006).10.1016/j.apradiso.2006.03.003Suche in Google Scholar

35. Zhang, J., Wang, X., Jin, C.: Synthesis and biodistribution of the 99mTc (CO)3-DEDT complex as a potential new radiopharmaceutical for brain imaging. J. Radioanal. Nucl. Chem. 272(1), 91 (2007).10.1007/s10967-006-6794-3Suche in Google Scholar

36. Erfani, M., Hassanzadeh, L., Ebrahimi, S. E. S., Shafiei, M.: Synthesis and biological evaluation of 99mTc (CO)3-OH-PP-CS2 for brain receptor imaging Iran. J. Nucl. Med. 20(1), 25 (2012).Suche in Google Scholar

37. Kuzniecky, R. I.: Neuroimaging of epilepsy: therapeutic implications. NeuroRx 2(2), 384 (2005).10.1602/neurorx.2.2.384Suche in Google Scholar

38. Suhara, T., Sudo, Y., Yoshida, K., Okubo, Y., Fukuda, H., Obata, T., Yoshikawa, K., Suzuki, K., Sasaki, Y.: Novel radioiodinated sibutramine and fluoxetine. Lancet. 351, 332 (1998).10.1016/S0140-6736(97)07336-4Suche in Google Scholar

39. Sanad, M. H., Sallam. Kh. M., Marzook, F. A., Abd-Elhaliem, S. M.: Radioiodination and biological evaluation of candesartan as a tracer for cardiovascular disorder detection. J. Label. Compd. Radiopharm. 59, 484 (2016).10.1002/jlcr.3435Suche in Google Scholar PubMed

40. Holman, B. L., Hellman, R. S., Goldsmith, S. J., Mena, I. G., Leveille, J., Gherardi, P. G., Moretti, J. L., Bischof-Delaloye, A., Hill, T. C., Rigo, P. M.: Biodistribution, dosimetry, and clinical evaluation of technetium-99m ethyl cysteinate dimer in normal subjects and in patients with chronic cerebral infarction. J. Nucl. Med. 30(6), 1018 (1989).Suche in Google Scholar

Received: 2016-10-14
Accepted: 2017-2-27
Published Online: 2017-4-19
Published in Print: 2017-9-26

©2017 Walter de Gruyter GmbH, Berlin/Boston

Artikel in diesem Heft

  1. Frontmatter
  2. Understanding the sorption behavior of Pu4+ on poly(amidoamine) dendrimer functionalized carbon nanotube: sorption equilibrium, mechanism, kinetics, radiolytic stability, and back-extraction studies
  3. Quaternary ammonium based task specific ionic liquid for the efficient and selective extraction of neptunium
  4. Synthesis and evaluation of N,N-di-alkyl-2-methoxyacetamides for the separation of U(VI) and Pu(IV) from nitric acid medium
  5. Synthesis, radiolabeling and biological evaluation of [125I]-1-[2-(benzylthio)ethyl]-4-(5-iodo-2-methoxyphenyl)piperazine as a new 5-HT1A receptor ligand
  6. Radiosynthesis and preclinical evaluation of [18F] 4-(2-fluoroethoxy)-2H-chromen-2-one as a novel myocardial perfusion imaging agent
  7. Radiocomplexation and bioevaluation of 99mTc nitrido-piracetam as a model for brain imaging
  8. Batch and column adsorption behaviors of Se(IV) and Te(IV) on organic and inorganic ion exchangers from HCl solutions
  9. Separation of 195(m,g),197mHg from bulk gold target by liquid-liquid extraction using hydrophobic ionic liquids
  10. Assessment of gamma radiation levels and natural radioactivity in soils along a subtropical river basin, China
  11. Natural radioactivity-based radiological hazards in soils of the islands: a case study from Eastern Turkey
  12. Book Review
  13. Nuclear and Radiochemistry: Fundamentals and Applications
https://doi.org/10.1515/ract-2016-2714
Schlagwörter für diesen Artikel
Piracetam; [99mTc≡N]2+core; labeling; biodistribution; brain; imaging

Artikel in diesem Heft

  1. Frontmatter
  2. Understanding the sorption behavior of Pu4+ on poly(amidoamine) dendrimer functionalized carbon nanotube: sorption equilibrium, mechanism, kinetics, radiolytic stability, and back-extraction studies
  3. Quaternary ammonium based task specific ionic liquid for the efficient and selective extraction of neptunium
  4. Synthesis and evaluation of N,N-di-alkyl-2-methoxyacetamides for the separation of U(VI) and Pu(IV) from nitric acid medium
  5. Synthesis, radiolabeling and biological evaluation of [125I]-1-[2-(benzylthio)ethyl]-4-(5-iodo-2-methoxyphenyl)piperazine as a new 5-HT1A receptor ligand
  6. Radiosynthesis and preclinical evaluation of [18F] 4-(2-fluoroethoxy)-2H-chromen-2-one as a novel myocardial perfusion imaging agent
  7. Radiocomplexation and bioevaluation of 99mTc nitrido-piracetam as a model for brain imaging
  8. Batch and column adsorption behaviors of Se(IV) and Te(IV) on organic and inorganic ion exchangers from HCl solutions
  9. Separation of 195(m,g),197mHg from bulk gold target by liquid-liquid extraction using hydrophobic ionic liquids
  10. Assessment of gamma radiation levels and natural radioactivity in soils along a subtropical river basin, China
  11. Natural radioactivity-based radiological hazards in soils of the islands: a case study from Eastern Turkey
  12. Book Review
  13. Nuclear and Radiochemistry: Fundamentals and Applications
Heruntergeladen am 13.4.2026 von https://www.degruyterbrill.com/document/doi/10.1515/ract-2016-2714/html
Button zum nach oben scrollen