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

Uygur, E; Parlak, Y; Karatay, KB; Sezgin, C; Gümüser, FG; Müftüler, FZB

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

Authors

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 [Tc-99m]Tc and the biological affinity of [Tc-99m]Tc-FTY-720 was assessed using in vitro methods. The radiochemical yield and stability of [Tc-99m]Tc-FTY-720 was over 95% during 4 h. [Tc-99m]Tc-FTY-720 showed uptake on the SH-SY5Y cell line.