268557-49-9Relevant articles and documents
Synthesis and evaluation of fluorinated fingolimod (FTY720) analogues for sphingosine-1-phosphate receptor molecular imaging by positron emission tomography
Shaikh, Rizwan S.,Schilson, Stefanie S.,Wagner, Stefan,Hermann, Sven,Keul, Petra,Levkau, Bodo,Sch?fers, Michael,Haufe, Günter
, p. 3471 - 3484 (2015/05/05)
Sphingosine-1-phosphate (S1P) is a lysophospholipid that evokes a variety of biological responses via stimulation of a set of cognate G-protein coupled receptors (GPCRs): S1P1-S1P5. S1P and its receptors (S1PRs) play important roles in the immune, cardiovascular, and central nervous systems and have also been implicated in carcinogenesis. Recently, the S1P analogue Fingolimod (FTY720) has been approved for the treatment of patients with relapsing multiple sclerosis. This work presents the synthesis of various fluorinated structural analogues of FTY720, their in vitro and in vivo biological testing, and their development and application as [18F]radiotracers for the study of S1PR biodistribution and imaging in mice using small-animal positron emission tomography (PET).
NEW LIGANDS FOR TARGETING OF S1P RECEPTORS FOR IN VIVO IMAGING AND TREATMENT OF DISEASES
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, (2014/06/25)
The present invention relates to novel compounds of formulae (I) and (II) which are useful in the prevention, treatment and diagnosis, in vivo diagnosis of diseases or disorders related to S1P receptors, in particular, in diseases which are connected to the regulatory function of sphingosine-1-phosphate (S1P) and its analogues, such as inflammation, pain, autoimmune diseases and cardiovascular diseases.
Synthesis, stability, and implications of phosphothioate agonists of sphingosine-1-phosphate receptors
Foss Jr., Frank W.,Clemens, Jeremy J.,Davis, Michael D.,Snyder, Ashley H.,Zigler, Molly A.,Lynch, Kevin R.,Macdonald, Timothy L.
, p. 4470 - 4474 (2007/10/03)
Phosphothioates may provide metabolic stability when compared to their phosphate counterparts, while retaining the potency and efficacy as agonists at sphingosine-1-phosphate (S1P) G-protein coupled receptors. Unlike their phosphate precursors, phosphothi