Chemical Name: (2S,3R,4E)-2-(Dimethylamino)-4-octadecene-1,3-diol
Biological ActivityCompetitive sphingosine kinase (SphK) inhibitor. Exhibits inhibitory activity in platelets and in cytosolic extracts from U937, Swiss 3T3 and PC12 cells. Selectively inhibits sphingosine phosphorylation; does not inhibit N-acylation, and displays no inhibitory effect on protein kinase C at concentrations that inhibit SphK. Increases the release of IL-1β and MCP-1 in cultured astrocytes; thought to mediate mechanical allodynia via this mechanism.
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Metabolomics implicates altered sphingolipids in chronic pain of neuropathic origin.
Patti et al.
N,N-dimethylsphingosine is a potent competitive inhibitor of sphingosine kinase but not of protein kinase C: modulation of cellular levels of sphingosine 1-phosphate and ceramide.
Edsall et al.
N,N-dimethylsphingosine inhibition of sphingosine kinase and sphingosine 1-phosphate activity in human platelets.
Yatomi et al.
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