A systematic evaluation of the potential of PCTA-NCS ligand as a bifunctional chelating agent for design of 177Lu radiopharmaceuticals

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• 作者：Usha Pandey ; Naresh Gamre ; Yogendra Kumar…
• 关键词：Therapeutic radiopharmaceuticals ; 177Lu ; Bifunctional chelating agent ; Trace metal ions
• 刊名：Journal of Radioanalytical and Nuclear Chemistry
• 出版年：2016
• 出版时间：January 2016
• 年：2016
• 卷：307
• 期：1
• 页码：187-194
• 全文大小：457 KB
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• 作者单位：Usha Pandey (1)
  Naresh Gamre (1)
  Yogendra Kumar (1)
  Priyalatha Shetty (1)
  Haladhar Dev Sarma (2)
  Ashutosh Dash (1)
  
  1. Isotope Production & Applications Division, Bhabha Atomic Research Centre (BARC), 400085, Mumbai, India
  2. Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre (BARC), 400085, Mumbai, India
  
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Chemistry
  Nuclear Chemistry
  Physical Chemistry
  Nuclear Physics, Heavy Ions and Hadrons
  Diagnostic Radiology
  Inorganic Chemistry
  
• 出版者：Akad茅miai Kiad贸, co-published with Springer Science+Business Media B.V., Formerly Kluwer Academic
• ISSN：1588-2780

文摘

This paper explores the utility of para isothiocyanato benzyl 3,6,9,15-tetraazabicyclo [9.3.1]pentadeca-1(15),11,13-triene-3,6,9-triacetic acid (PCTA-NCS) as a bifunctional chelating agent for 177Lu in comparison to para isothiocyanato benzyl 1,4,7,10-tetra aza cyclododecane tetraacetic acid (DOTA-NCS). The 177Lu-PCTA-NCS complex could be obtained in high radiolabeling yields at ambient temperature and exhibited excellent stability in vitro. Influence of trace metal ions on the radiolabeling yields was also evaluated. Biodistribution studies revealed no significant retention of 177Lu-PCTA-NCS in any vital organ at 24 h p.i. It could be concluded from our study that PCTA-NCS could be a potential BFCA for design of 177Lu radiopharmaceuticals.