Pharmacological characterization of human S1P 4 using a novel radioligand, [4,5‐ 3 H]‐dihydrosphingosine‐1‐phosphate

Sphingosine‐1‐phosphate (S1P) is a bioactive lipid that affects a variety of cellular processes through both its actions as a second messenger and via activation of a family of G protein‐coupled receptors (S1P 1–5 ). The study of S1P receptor pharmacology, particularly S1P 4 , has been hindered by t...

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Published inBritish journal of pharmacology Vol. 142; no. 5; pp. 851 - 860
Main Authors Fossetta, James, Deno, Gregory, Gonsiorek, Waldemar, Fan, Xuedong, Lavey, Brian, Das, Pradip, Lunn, Charles, Zavodny, Paul J, Lundell, Daniel, Hipkin, R William
Format Journal Article
LanguageEnglish
Published 29.01.2009
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Summary:Sphingosine‐1‐phosphate (S1P) is a bioactive lipid that affects a variety of cellular processes through both its actions as a second messenger and via activation of a family of G protein‐coupled receptors (S1P 1–5 ). The study of S1P receptor pharmacology, particularly S1P 4 , has been hindered by the lack of high‐affinity radioligands with good specific activity. The studies presented herein characterize [ 3 H]DH‐S1P as a stable, high‐affinity radioligand for S1P 4 pharmacology. Using a transfected Ba/F3 cell line selected for high hS1P 4 surface expression, we compared the consequences of different cellular backgrounds and commercial sources of sphingophospholipids on S1P 4 characterization. The development and subsequent use of the assay described has enabled us to extensively and definitively characterize the pharmacology of the human S1P 4 receptor. British Journal of Pharmacology (2004) 142 , 851–860. doi: 10.1038/sj.bjp.0705856
ISSN:0007-1188
1476-5381
DOI:10.1038/sj.bjp.0705856