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

Adam J. Rosenberg; Hui Liu; Zhude Tu

doi:10.1016/j.apradiso.2015.04.010

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

Adam J. Rosenberg
, Hui Liu
, Zhude Tu

Research output: Contribution to journal › Article › peer-review

21 Scopus citations

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 [³²P]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.

Original language	English
Pages (from-to)	5-9
Number of pages	5
Journal	Applied Radiation and Isotopes
Volume	102
DOIs	https://doi.org/10.1016/j.apradiso.2015.04.010
State	Published - Aug 1 2015

Keywords

Competitive binding assay
Phosphorus-32
Radioligand
Sphingosine 1-phosphate
Sphingosine 1-phosphate Receptors
Sphingosine kinase 1

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10.1016/j.apradiso.2015.04.010

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title = "A practical process for the preparation of [32P]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 [32P]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.",

keywords = "Competitive binding assay, Phosphorus-32, Radioligand, Sphingosine 1-phosphate, Sphingosine 1-phosphate Receptors, Sphingosine kinase 1",

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AU - Rosenberg, Adam J.

AU - Liu, Hui

AU - Tu, Zhude

PY - 2015/8/1

Y1 - 2015/8/1

N2 - 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 [32P]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.

AB - 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 [32P]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.

KW - Competitive binding assay

KW - Phosphorus-32

KW - Radioligand

KW - Sphingosine 1-phosphate

KW - Sphingosine 1-phosphate Receptors

KW - Sphingosine kinase 1

UR - https://www.scopus.com/pages/publications/84928580233

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DO - 10.1016/j.apradiso.2015.04.010

M3 - Article

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AN - SCOPUS:84928580233

SN - 0969-8043

VL - 102

SP - 5

EP - 9

JO - Applied Radiation and Isotopes

JF - Applied Radiation and Isotopes

ER -

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

Abstract

Keywords

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