A practical process for the preparation of [(32)P]S1P and binding assay for S1P receptor ligands.
Sphingosine-1-phosphate receptors (S1PRs) are important regulators of vascular permeability, inflammation, angiogenesis and vascular maturation. Identifying a specific S1PR PET radioligand is imperative, but it is hindered by the complexity and variability of current for binding affinity measurement procedures. Herein, we report a streamlined protocol for radiosynthesis of [(32)P]S1P with good radiochemical yield (36-50%) and high radiochemical purity (>99%). We also report a reproducible procedure for determining the binding affinity for compounds targeting S1PRs in vitro.
Department of Radiology, Washington University School of Medicine, 510 South Kingshighway Boulevard, St. Louis, MO 63110, USA.
Adam J
AJ
Rosenberg
Department of Radiology, Washington University School of Medicine, 510 South Kingshighway Boulevard, St. Louis, MO 63110, USA.
Hui
H
Liu
Department of Radiology, Washington University School of Medicine, 510 South Kingshighway Boulevard, St. Louis, MO 63110, USA. Electronic address: tuz@mir.wustl.edu.
Zhude
Z
Tu
D001667:Binding, Competitive; D008024:Ligands; D008246:Lysophospholipids / Q000378:metabolism*; D010761:Phosphorus Radioisotopes / Q000378:metabolism*; D049349:Receptors, Lysosphingolipid / Q000378:metabolism*; D013110:Sphingosine / Q000031:analogs & derivatives* / Q000378:metabolism
D008024:Ligands; D008246:Lysophospholipids; D010761:Phosphorus Radioisotopes; D049349:Receptors, Lysosphingolipid; C060506:sphingosine 1-phosphate; D013110:Sphingosine
Competitive binding assay; Phosphorus-32; Radioligand; Sphingosine 1-phosphate; Sphingosine 1-phosphate Receptors; Sphingosine kinase 1