A practical process for the preparation of [(32)P]S1P and binding assay for S1P receptor ligands.

Abstract

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.

• Authors: Adam J Rosenberg, Hui Liu, Zhude Tu
• Journal: Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine (Appl Radiat Isot) Vol. 102 Pg. 5-9 (Aug 2015) ISSN: 1872-9800 [Electronic] England
• PMID: 25931137 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, U.S. Gov't, Non-P.H.S.)
• Copyright: Copyright © 2015 Elsevier Ltd. All rights reserved.

Chemical References

• Ligands
• Lysophospholipids
• Phosphorus Radioisotopes
• Receptors, Lysosphingolipid
• sphingosine 1-phosphate
• Sphingosine

Topics

• Binding, Competitive
• Ligands
• Lysophospholipids (metabolism)
• Phosphorus Radioisotopes (metabolism)
• Receptors, Lysosphingolipid (metabolism)
• Sphingosine (analogs & derivatives, metabolism)