Radiolabeling fingolimod with technetium-99 m and evaluating its biological affinity by in vitro method

UYGUR E., PARLAK Y., Karatay K., Sezgin C., GÜMÜŞER F. G., Biber Müftüler F.

Journal of Radioanalytical and Nuclear Chemistry, vol.332, no.11, pp.4781-4789, 2023 (SCI-Expanded, Scopus) identifier identifier

  • Publication Type: Article / Article
  • Volume: 332 Issue: 11
  • Publication Date: 2023
  • Doi Number: 10.1007/s10967-023-08907-3
  • Journal Name: Journal of Radioanalytical and Nuclear Chemistry
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, Aerospace Database, Analytical Abstracts, Biotechnology Research Abstracts, CAB Abstracts, Chemical Abstracts Core, Chimica, Communication Abstracts, Food Science & Technology Abstracts, INSPEC, Metadex, Pollution Abstracts, Public Affairs Index, Veterinary Science Database, Civil Engineering Abstracts
  • Page Numbers: pp.4781-4789
  • Keywords: Fingolimod, Parkinson's disease, Multiple sclerosis, Technetium-99 m [Tc-99m]Tc
  • Manisa Celal Bayar University Affiliated: Yes

Abstract

Fingolimod (FTY-720) is the first oral medication approved by the food and drug administration (FDA) for the treatment of multiple sclerosis. It acts on the central nervous system by crossing the blood–brain barrier and binding to sphingosine-1-phosphate receptors (S1PRs). FTY-720 protects against neural damage caused by mitochondrial dysfunction and cytotoxicity by modulating S1PR1. In this study, FTY-720 was radiolabeled with technetium-99 m [99mTc]Tc and the biological affinity of [99mTc]Tc-FTY-720 was assessed using in vitro methods. The radiochemical yield and stability of [99mTc]Tc-FTY-720 was over 95% during 4 h. [99mTc]Tc-FTY-720 showed uptake on the SH-SY5Y cell line.