26207-06-7Relevant articles and documents
Novel Potent Selective Orally Active S1P5 Receptor Antagonists
Ma, Bin,Guckian, Kevin M.,Liu, Xiao-Gao,Yang, Chunhua,Li, Bing,Scannevin, Robert,Mingueneau, Micha?l,Drouillard, Annabelle,Walzer, Thierry
supporting information, (2021/02/01)
S1P5 is one of the five sphingosine-1-phosphate (S1P) receptors which play important roles in immune and CNS cell homeostasis, growth, and differentiation. Little is known about the effect of modulation of S1P5 due to the lack of S1P5 specific modulators with suitable druglike properties. Here we describe the discovery and optimization of a novel series of potent selective S1P5 antagonists and the identification of an orally active brain-penetrant tool compound 15.
S1P MODULATING AGENTS
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Page/Page column 41, (2014/08/19)
Compounds of formula (I) can modulate the activity of one or more S 1P receptors. Sphingosine 1-phosphate (S IP) is a lysophospholipid mediator that evokes a variety of cellular responses by stimulation of five members of the endothelial cell differentiation gene (EDG) receptor family, namely S1P1, S1P2, S1P3, S1P4, and S1P5 (formerly EDG1, EDG5, EDG3, EDG6 and EDG8). The EDG receptors are G-protein coupled receptors (GPCRs) and on stimulation propagate second messenger signals via activation of heterotrimeric G-protein alpha (Ga.) subunits and beta-gamma (G()y) dimers.
BICYCLIC ARYL SPHINGOSINE 1-PHOSPHATE ANALOGS
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Page/Page column 139-140, (2011/02/24)
Compounds that have agonist activity at one or more of the SlP receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at SlP receptors.