Literature DB >> 25931137

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

Adam J Rosenberg1, Hui Liu1, Zhude Tu2.   

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.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

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

Mesh：

Substances：

Year:  2015        PMID： 25931137      PMCID： PMC4457593          DOI： 10.1016/j.apradiso.2015.04.010

Source DB:  PubMed          Journal:  Appl Radiat Isot        ISSN： 0969-8043            Impact factor:   1.513


  28 in total

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Authors:  J R Van Brocklyn; S Spiegel
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6.  Enhancement of sphingosine 1-phosphate-induced migration of vascular endothelial cells and smooth muscle cells by an EDG-5 antagonist.

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Journal:  Biochem Biophys Res Commun       Date:  2002-12-06       Impact factor: 3.575

Review 7.  The structure and function of the S1P1 receptor.

Authors:  Catherine O'Sullivan; Kumlesh K Dev
Journal:  Trends Pharmacol Sci       Date:  2013-06-11       Impact factor: 14.819

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Authors:  Toshikazu Hakogi; Toshihiko Shigenari; Shigeo Katsumura; Takamitsu Sano; Takayuki Kohno; Yasuyuki Igarashi
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  10 in total

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3.  A potent and selective C-11 labeled PET tracer for imaging sphingosine-1-phosphate receptor 2 in the CNS demonstrates sexually dimorphic expression.

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Journal:  Bioorg Med Chem       Date:  2019-06-29       Impact factor: 3.641

5.  Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2.

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6.  Syntheses and in vitro evaluation of new S1PR1 compounds and initial evaluation of a lead F-18 radiotracer in rodents.

Authors:  Zonghua Luo; Adam J Rosenberg; Hui Liu; Junbin Han; Zhude Tu
Journal:  Eur J Med Chem       Date:  2018-03-14       Impact factor: 6.514

7.  Design, Synthesis, and In Vitro and In Vivo Evaluation of an (18)F-Labeled Sphingosine 1-Phosphate Receptor 1 (S1P1) PET Tracer.

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8.  A promising carbon-11-labeled sphingosine-1-phosphate receptor 1-specific PET tracer for imaging vascular injury.

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9.  Synthesis and characterization of [125I]TZ6544, a promising radioligand for investigating sphingosine-1-phosphate receptor 2.

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  10 in total

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