The use of diaminodithiol for labeling small molecules with technetium-99m |
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| Affiliation: | 1. Sydney School of Public Health, The University of Sydney, Sydney, Australia;2. Centre for Kidney Research, The Children’s Hospital at Westmead, Sydney, Australia;3. College of Medicine and Public Health, Flinders University, Adelaide, South Australia, Australia;4. Division of Nephrology, Department of Pediatrics, All India Institute of Medical Sciences, New Delhi, India;5. Department of Pediatrics and Child Health, The Children''s Hospital Research Institute of Manitoba, University of Manitoba, Winnipeg, Manitoba, Canada;6. Department of Pediatrics, University of British Columbia, Vancouver, British Columbia, Canada;7. Division of Nephrology, Department of Pediatrics, University of Michigan, Ann Arbor, Michigan, USA;8. University College London Department of Renal Medicine, Great Ormond Street Hospital for Children, National Health Service Foundation Trust, London, UK;9. Department of Pediatrics, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, Singapore;10. Department of Pediatric Nephrology, Emma Children''s Hospital Academic Medical Center, Amsterdam, The Netherlands;11. Department of Nephrology, SickKids, Toronto, Ontario, Canada;12. Department of Paediatric Nephrology and National Institute for Health Research/Wellcome Trust Clinical Research Facility University of Manchester, Manchester Academic Health Science Centre, Royal Manchester Children’s Hospital, Manchester, UK;13. Department of Pediatrics, Perelman School of Medicine at the University of Pennsylvania, Children’s Hospital of Philadelphia, Philadelphia, Pennsylvania, USA;14. Department of Pediatrics, Section of Nephrology, University of Calgary, Calgary, Alberta, Canada;15. Division of Pediatric Nephrology, The Johns Hopkins University School of Medicine, Baltimore, Maryland, USA;16. Department of Nephrology, Princess Alexandra Hospital, Brisbane, Queensland, Australia;17. Australasian Kidney Trials Network, The University of Queensland, Brisbane, Queensland, Australia;18. Division of Nephrology and Hypertension, Lundquist Institute at Harbor–University of California Los Angeles Medical Center, Torrance, California, USA;19. Center of Pediatrics, Institute of Clinical Medicine, Faculty of Medicine, Vilnius University, Vilnius, Lithuania;20. Sheffield Teaching Hospitals, National Health Service Foundation Trust, Sheffield, UK;21. Department of Nephrology and Murdoch Children''s Research Institute, Royal Children''s Hospital, Melbourne, Victoria, Australia;22. Department of Pediatrics, University of Melbourne, Melbourne, Victoria, Australia;23. Child and Adolescent Renal Service, Queensland Children’s Hospital, Brisbane, Queensland, Australia;24. Department of Pediatrics, Loma Linda University Children’s Hospital, Loma Linda, California, USA;25. Department of Pediatrics, Division of Nephrology, University of California Los Angeles, David Geffen School of Medicine at University of California Los Angeles, Los Angeles, California, USA;26. Rady Children’s Hospital, University of California at San Diego, San Diego, California, USA;1. Laboratoire Lagrange, Université Côte d’Azur, Observatoire de la Côte d’Azur, CNRS, CS 34229, 06304 Nice Cedex 4, France;2. JHU/APL, USA;3. ESA/ESAC, Spain;4. Ondrejov Obs., Czech Republic;5. TU Braunschweig, Germany;6. Open University, UK;7. Royal Observatory of Belgium, Belgium;8. Aristotle University of Thessaloniki, Greece;9. Max-Planck Institute, Göttingen, Germany;10. German Aerospace Center, DLR, Cologne, Germany;11. UVSQ (UPSay), UPMC (Sorbonne Univ.), CNRS/INSU, LATMOS-IPSL, Guyancourt, France;12. Univ. Grenoble Alpes, IPAG, CNRS, IPAG, Grenoble, France;13. ESA/Hq, Paris, France;14. JPL, Pasadena, USA;15. Univ. Maryland, College Park, USA;p. Lowell Observatory, Flagstaff, USA;q. Universidad de Alicante, Spain;1. Sydney School of Public Health, The University of Sydney, Sydney, Australia;2. Centre for Kidney Research, The Children’s Hospital at Westmead, Sydney, Australia;3. College of Medicine and Public Health, Flinders University, Adelaide;4. Department of Nephrology, Princess Alexandra Hospital, Faculty of Medicine, University of Queensland, Brisbane, Australia;5. Department of Pediatrics, BC Children''s Hospital and University of British Columbia, Vancouver, Canada;6. Child and Adolescent Renal Service, Lady Cilento Children’s Hospital and University of Queensland, Brisbane, Australia;7. Pediatrics-Renal, Texas Children’s Hospital/Baylor College of Medicine, Houston, TX;8. Department of Nephrology, Royal Children’s Hospital Melbourne, University of Melbourne and Murdoch Children’s Research Institute, Victoria Australia;9. Department of Pediatrics, University of Melbourne and Murdoch Children’s Research Institute, Victoria Australia;10. Selzman Institute for Kidney Health, Section of Nephrology, Baylor College of Medicine, Houston, TX;11. UCL Centre for Nephrology and Great Ormond Street Hospital for Children NHS Foundation Trust, London, United Kingdom;12. Department of Pediatrics and Child Health, The Children’s Hospital Research Institute of Manitoba, University of Manitoba, Winnipeg, Canada;13. Departments of Pediatrics and Epidemiology, Perelman School of Medicine, Division of Nephrology, The Children’s Hospital of Philadelphia, Philadelphia, PA;14. Department of Pediatrics, School of Medicine, University of Michigan, Ann Arbor, MI;15. Division of Nephrology and Hypertension, Cincinnati Children''s Hospital Medical Center, Cincinnati, OH;16. Department of Pediatric Nephrology, Emma Children''s Hospital AMC Academic Medical Center, Amsterdam, the Netherlands;17. Department of Pediatrics, Section of Nephrology, University of Calgary, Calgary, Canada;18. Division of Nephrology, Department of Pediatrics, All India Institute of Medical Sciences, New Delhi, India;19. Department of Pediatric Nephrology and NIHR/Wellcome Trust Clinical Research Facility, University of Manchester, Manchester Academic Health Science Centre, Royal Manchester Children’s Hospital, Manchester, United Kingdom;20. Department of Pediatrics, Yong Loo Lin School of Medicine, National University of Singapore, Singapore;21. Department of Pediatrics, Division of Nephrology, Toronto Hospital for Sick Children, University of Toronto, Toronto, Canada;1. Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, People’s Republic of China;2. Laboratory for Marine Drugs and Bioproducts of Qingdao National Laboratory for Marine Science and Technology, 266237, People’s Republic of China;1. Department of Medicinal Chemistry, Student Research Committee, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran;2. Department of Toxicology and Pharmacology, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran;3. Diabetes Research Center, Mazandaran University of Medical Sciences, Sari, Iran;4. Department of Clinical Biochemistry, School of Medicine, Shahid Beheshti University of Medical Sciences (SBMU), Tehran, Iran;5. Molecular and Cell Biology Research Center, Mazandaran University of Medical Sciences, Sari, Iran;6. Department of Medicinal Chemistry, School of Pharmacy, Ardabil University of Medical Sciences, Ardabil, Iran;7. Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran |
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| Abstract: | To investigate the labeling of small molecules with 99mTc by the bifunctional chelate approach, we have synthesized both a fatty acid and an estrone derivative containing a chelator of the N2S2 type. In the case of the fatty acid, this was a diaminodithiol (DADT) while for the estrone, a diaminodisulfide (DADS) was attached. The estrone derivative (5-(2-methylene estrone 3-methyl ether)-3,3,10,10-tetramethyl-1, 2-dithia-5,8-diazacyclodecane hydrochloride, DADS-E) was prepared by alkylation of DADS while the fatty acid derivative (N-(11-undecanoic acid)-N,N′-bis(2-methyl-2-mercaptopropyl) ethylenediamine hydrochloride, DADT-FA) was synthesized by alkylation of DADS followed by reduction. DADS-E was labeled in ethanol at elevated temperatures while DADT-FA was labeled at room temperature, both by stannous reduction. Paper chromatography showed both to be labeled and reverse-phase HPLC showed multiple peaks for both. Serum stability studies were performed by incubation at 37 °C with aliquots removed at 1 min and 1 day for analysis by size-exclusion HPLC. Initially, little pertechnetate or binding to serum proteins was observed whereas after 1 day the majority of activity in both cases was protein bound with 20 and 38% pertechnetate appearing for DADT-FA and DADS-E respectively. In conclusion, small biologically active molecules may be labeled with 99mTc through an attached diaminodithiol or diaminodisulfide group. |
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